Tag: M.W:300-400

1001180-21-7, (R)-tert-Butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1001180-21-7, A 3000 L glass-lined reactor was evacuated and filled with nitrogen to normal pressure 3 times. Water (660.0 kg) was added into the reactor while maintaining the temperature in the range of 20-30 C. The stirrer was started, followed by the addition of potassium dihydrogen phosphate (9.2 kg), dipotassium phosphate (23.7 kg) and glucose (78.5 kg). The mixture was stirred until solid dissolved completely. Then 30.1 kg of this buffer mixture was discharged into a 50 L drum for future use. To the reactor was added (R)-tert-butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate (66.0 kg) and PEG400 (732.6 kg) and the mixture was heated to about 30-35 C. Maintaining the temperature at 30-35 C., a mixture of buffer solution (20.0 kg), KRED-101 (2.4 kg), GDH (3.4 kg) and NADP (2.2 kg) was added into the mixture. The mixture was then maintained at 32-37 C. for reaction while controlling the pH at 6.8-7.1. After about 6 h, the mixture was monitored by TLC and HPLC until ketone starting substrate was ?1.0%. During the reaction, potassium hydroxide solution (total 46.2 kg) and extra enzyme buffer solution prepared with purified water (5.0 kg), KRED-101 (0.24 kg), GDH (0.34 kg) and NADP (0.22 kg) were added. To a glass-lined reactor, isopropyl acetate (1148.6 kg) was added. The reaction mixture from the previous paragraph was added to the reactor in three portions. Each time, it was stirred for 15-20 min and held for at least 0.5 h before separation at 20-30 C. This extraction process was repeated three times. The organic phases were combined. At 20-30 C., the combined organic phases were washed with purified water (329.3 kg). It was stirred for 25-30 min and held for at least 30 min before separation. The organic phase was left in the reactor and the washing process was repeated. The organic phase was decolorized with active carbon (6.6 kg) and stirred for 1-1.5 h. The mixture was filtered via a Nutsche filter. The cake was washed with isopropyl acetate (57.5 kg). The filtrates were combined. The filtrate was then transferred into a thin film evaporator and concentrated at ?55 C. under reduced pressure until 500-600 L remained. The concentrated mixture was filtered and transferred into a glass-lined reactor, then concentrated at ?55 C. under reduced pressure until 50-60 L remained. The mixture was then heated to 50-55 C. and stirred at this temperature for 0.5-1.5 h under nitrogen. n-Heptane (277.2 kg) was added into the mixture at the rate of 20-30 kg/h while maintaining the temperature at 50-55 C. The mixture was then cooled to 20-30 C. at the rate of 5-10 C./h. The mixture was stirred at 20-30 C. for 1 h, then heated to 50-55 C. and stirrer for 1-2 h, and then cooled to 15-20 C. at a rate of 5-10 C./h for crystallization. It was sampled to be analyzed by HPLC every 1-2 h until wt % of the mother liquid was ?3% or the change of the wt % between consecutive samples was ?0.5%. The mixture was then filtered with a centrifuge. The filter cake was washed with n-heptane (45.0 kg). The filtrate was transferred into a glass-lined reactor and concentrated at ?45 C. under reduced pressure (?-0.06 MPa) until no more distillate was observed (approximately 20 L remained). Isopropyl acetate (20.0 kg) was added, the mixture was heated to 45-55 C. and stirred for 0.5-1 h. The mixture was dried at 40-50 C. to give tert-butyl 4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate as grey solid (50.65 kg, 76.3% yield), HPLC rt=18.93 min, 99.9% pure, 100% de, 100% ee. The HPLC conditions are given in Table 1 below.

As the paragraph descriping shows that 1001180-21-7 is playing an increasingly important role.

Reference£º
Patent; Genetech, Inc.; Babu, Srinivasan; Gosselin, Francis; Ran, Yingqing; Remarchuk, Travis; Savage, Scott J.; Stults, Jeffrey; Yajima, Herbert; US2015/99880; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.113028-17-4,Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate,as a common compound, the synthetic route is as follows.

Ethyl-6-fluoro-1 -methyl-4-oxo-7-(1 -piperazinyl)-4H-(1 ,3)-thiazeto-[3,2-a]-quinoline-3- carboxylate (100 gms, 0.265 moles) was stirred in water (600 ml) at 25-30C. To this potassium hydroxide solution (50 gms of potassium hydroxide flakes is dissolved in 200 ml of water) was added and the reaction mass was heated to 80-85C. The contents were stirred for 1 hour and after completion of reaction, the reaction mass was cooled to 25-30C. The pH of the reaction mass was adjusted to 6.5-7.0 using 1:1 aqueous acetic acid solution. The contents were stirred at room temperature for 1 hour. The precipitated solid was filtered, washed with water (2 x 100 ml). The solid was slurried in methanol (300 ml) for 1 hour at 25-30C, filtered, washed with methanol (2 x 50 ml) and dried under vacuum at 70-75C to yield the title compound [90 gms, 97% yield, 96% HPLC purity].

113028-17-4, As the paragraph descriping shows that 113028-17-4 is playing an increasingly important role.

Reference£º
Patent; CIPLA LIMITED; PATHI, Srinivas Laxminarayan; RAO, Dharmaraj Ramachandra; KANKAN, Rajendra; CHINIMILLI, Venugopalarao; CURTIS, Philip Anthony; WO2012/1357; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

112257-12-2, tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step G. 6-Chloro-12-(2-oxo-2-piperazin-1-ylethoxy)-2,4,8,22-tetraazatetracyclo[14.3.1.1(3,7).1(9,13)]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene bis(trifluoroacetate) 6-Chloro-2,4,8,22-tetraazatetracyclo[14.3.1.1(3,7).1(9,13)]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaen-12-ol (100 mg, 0.30 mmol), potassium carbonate (102 mg, 0.74 mmol), and tert-butyl 4-(bromoacetyl)piperazine-1-carboxylate (181 mg, 0.59 mmol) were stirred in N,N-dimethylformamide (2 mL) for 16 hours at 70 C. Purification by preparative LCMS (pH 2) and treatment with 1:1 trifluoroacetic acid and methylene chloride followed by evaporation gave the desired compound (33 mg, 19%). LCMS for C24H26ClN6O2 (M+H)+: m/z=465.2.

112257-12-2, 112257-12-2 tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate 15829155, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; INCYTE CORPORATION; US2009/286778; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

Example 36 Preparation of N -(8-fluoro-2-methylimidazo[1,2-a]pyridin-6-yl)-4-(piperazin-1-yl) benzamide hydrochloride To a solution of 4-(4-(tert-butoxycarbonyl)piperazin-1-yl)benzoic acid (commercial) (109 mg,357 flmol) in N,N-dimethylformamide (1.00 ml) under nitrogen at room temperature, wereadded HA TU ( 0-(7-azabenzotriazol-1-yl)-N ,N ,N’ ,N’-tetramethyluronium hexafluorophosphate)(204 mg, 536 flmol) and N-ethyldiisopropylamine (185 mg, 243 f..Ll, 1.43 mmol). After 5 minutesstirring at room temperature, 8-fluoro-2-methyl-imidazo[1,2-a]pyridin-6-ylamine hydrochloride (Example B.4) (72 mg, 357 flmol) was added. The mixture was stirred at room temperature for21 hours and then at 60C for 2 hours. The solvent was removed in vacuo. The residue was taken in a saturated aqueous solution of bicarbonate and extracted three times with ethyl acetate. The combined extracts were dried over sodium sulfate, filtered and concentrated in vacuo. The crude oil was purified on silica gel (Eluent: heptane/ethyl acetate 0 to 10%) to provide 78 mg of tert-butyl 4-(4-(8-fluoro-2-methylimidazo[1,2-a]pyridin-6-ylcarbamoyl)phenyl)piperazine-1-carboxylate. To a suspension of this compound (40 mg, 88.2 flmol) in methanol (400 f..Ll) was added HC14M in dioxane (221 f..Ll, 882 flmol). The light yellow suspension was stirred at roomtemperature for 17 hours. The solid was filtered, washed with ether and hexane and dried toprovide 25 mg (72.7 %) of the title compound as a light yellow solid., 162046-66-4

162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; PTC THERAPEUTICS INC.; DAKKA, Amal; GREEN, Luke; KARP, Gary; NARASIMHAN, Jana; NARYSHKIN, Nikolai; PINARD, Emmanuel; QI, Hongyan; RATNI, Hasane; RISHER, Nicole; WEETALL, Marla; WOLL, Matthew; WO2014/209841; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

112984-60-8, 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Synthesis of 6-FIisoro-7-{4-[3-hydroxy-4-(2-methyl-5-iiitro- imida2o-l-yl)-buty|-piperazin-l-yi}-1 -niethyl-4-ox0-4H~2 hia-8b-a2a- cyclobiita[a]naphthaIeiie-3-carboxySic acid (116): To a stirred solution of 6- Fluoro- I -methyl-4-oxo-7-piperazin-l -yi-4H-2-thia-8b-aza- cycIobuta a]naphthalene-3-carboxyIie acid, (III) (3g, 8.6 mmol) in DMF (30ral) was added potassium carbonate ( S .20g, 8.6 mmol) followed by addition of compound (II) (2g, 7.2 mmol) and the reaction mixture was stirred at RT for 16h. The reaction mixture was diluted with ethyl acetate, washed twice with water and finally dried over sodium sulphate to obtain the crude mass. The crude was purified by flash column chromatography while eiuting with 3-5% methanol/dichloromethane mixture to obtain the pure compound (116) with 20% isolated yield. -NMR (400 MHz, DMSO) deltarhorhoetaiota: 1.61-1.68 (2H, m, CH2), 2.12 (3H, d, J = 6 Hz, CH3), 2.46 (3H, s, CH3), 2.57 (4H, m, 2 x CH2), 3.2 (4H, m, 2 x CH2), 3.8-4.1 (2H, m, 2 x’ CH2N), 4.44(1H, m, CHOH), 5.2 (1H, bs, CHOH), 6.4 (1H, q, Ji = 5.6Hz, J2 = 1 1.6Hz, CHSN) 6.91 (1 H, d, J = 7, Ar-H), 7.78 (1H, d, J= 13.6 Hz, Ar-H). 8.04 (I H, s, Ar-H). ESI-MS (m/z): 547.08(M+H)+., 112984-60-8

112984-60-8 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid 124225, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; CHAWRAI, Suresh Rameshlal; GHOSH, Shamik; GHOSH, Sumana; JAIN, Nilu; SADHASIVAM, Suresh; BUCHTA, Richard; BHATTACHARYYA, Anamika; WO2015/114666; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,162046-66-4

To a stirred solution of 5 -(2-aminothiazol-5 -yl)sulfanyl -2-methoxy-4-methyl- benzoic acid (530.46 mg, 1.79 mmol), 1-piperazin-1-ylprop-2-en-1-one; 2,2,2-trifluoroacetic acid (455 mg, 1.79 mmol) and DIPEA (3.93 mL, 8.95 mmol) in DMF (5 mL) was added HATU (680.56 mg, 1.79 mmol). After 2 h, 4-(4-tert-butoxycarbonylpiperazin-1-yl)benzoic acid (1.37 g, 4.47 mmol), HATU (1.70 g, 4.47 mmol) and DIPEA (3.93 mL, 8.95 mmol) inDMF (5 mL) was added. The resulting mixture was heated to 80 oC. After 4 h, the reaction mixture was extracted with EtOAc (2 x 100 mL), 2 M aq. citric acid (2 x 200 mL) and brine (100 mL). The combined organic extracts were dried over Na2504, filtered and concentrated. Silica gel chromatography (DCM, MeOH) afforded the title compound (471 mg). MS (ES) m/z 707.3 (M+H).

162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CORVUS PHARMACEUTICALS, INC.; HUDSON, Ryan; BEAUSOLEIL, Anne-Marie; (616 pag.)WO2018/89261; (2018); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.171504-98-6,Methyl 1,4-Bis(Boc)-2-piperazinecarboxylate,as a common compound, the synthetic route is as follows.

(B) 1,4-Di-(N-tert-Butoxycarbonyl)-2-Piperazinecarboxylic Acid A solution of 1 N sodium hydroxide (1.2 mL) was added to a solution methyl 1,4-di-(N-tert-butoxycarbonyl)-2-piperazinecarboxylate (A, 290 mg) in methanol (10 mL). The mixture was stirred at room temperature for 12 hr and evaporated in vacuo. The residue was diluted with water and washed with ether. The aqueous layer was acidified with 10% citric acid and extracted with ethyl acetate. The organic layer was washed with brine, dried over anhydrous sodium sulfate, and evaporated in vacuo to give the title compound (230 mg) as a colorless foam: 1H NMR (400 MHz, CDCl3) delta 1.44 (s,18H) and 4.56-4.75 (m, 1H)., 171504-98-6

The synthetic route of 171504-98-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Microcide Pharmaceuticals, Inc.; US6399629; (2002); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1228780-72-0, 1-((4′-Chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Under nitrogen protection, Compound 20 (1.0 g, 3.13 mmol), Compound 1 (0.9 g, 3.13 mmol) and dipotassium hydrogen phosphate (1.10 g, 6.26 mmol) Add to a solution of dimethyl sulfoxide (DMSO, 25 ml), The reaction solution was reacted at 140 C for 12 h, and cooled to room temperature. The reaction was quenched with water (50 mL). Dry over anhydrous sodium sulfate, remove the solvent,The concentrate is subjected to column separation (eluent: petroleum ether/ethyl acetate (v/v) = 3:1), Obtained 1.4 g of a yellow oil, The yield was 76%.

1228780-72-0, As the paragraph descriping shows that 1228780-72-0 is playing an increasingly important role.

Reference£º
Patent; Shenzhen Tajirui Bio-pharmaceutical Co., Ltd.; Wang Yihan; Liu Zhiqiang; (35 pag.)CN108658983; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

181955-79-3, 1,4-Di-Boc-piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1,4-bis(tert-butoxycarbonyl)piperazine-2-carboxylic acid (4.88 g, 14.7 mmol) in DMF (49 mL) was added K2CO3 (2.65 g, 19.2 mmol), and the mixture cooled to 0 C. To the mixture was then slowly added methyl iodide (1.38 mL, 22.1 mmol). The reaction stirred was stirred at room temperature for 18 hours and quenched with saturated aqueous NH4Cl (100 mL). The mixture was diluted with water and extracted with EtOAc twice. The combined organic layers were washed with water and brine, dried over Na2SO4, filtered and concentrated in vacuo. The residue was purified by column chromatography on SiO2 (Hex:EtOAc=7:1 to 5:1 to 3:1) to afford 1,4-di-tert-butyl 2-methyl piperazine-1,2,4-tricarboxylate (5.09 g, 100%) as a pale brown viscous oil. 1H-NMR (CDCl3, Varian, 400 MHz): delta 1.44 (18H, s), 2.80 (1H, br. s), 3.12-3.24 (1H, m), 3.21 (1H, br. s), 3.74 (3H, s), 3.80-4.10 (2H, m), 4.48-4.73 (2H, m).

181955-79-3, The synthetic route of 181955-79-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; HANDOK INC.; CMG Pharmaceutical Co., Ltd.; Kim, Moonsoo; Lee, Chaewoon; Lee, Gilnam; Yoon, Cheolhwan; Seo, Jeongbeob; Kim, Jay Hak; Lee, Minwoo; Jeong, Hankyul; Choi, Hyang; Jung, Myung Eun; Lee, Ki Nam; Kim, Hyun Jung; Kim, Hye Kyoung; Lee, Jae Il; Lee, MinWoo; Kim, Misoon; Choi, Soongyu; (124 pag.)US2016/168156; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.149057-19-2,4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

Stage 1: 4-Benzyl 1 -tert-butyl 2-cyclopentyl piperazi ne-i ,2,4-tricarboxylate 4-[(Benzyloxy)carbonyl]- 1 -(tert-butoxycarbonyl)piperazi ne-2-carboxylic acid (9.96 g, 27 mmol) was dissolved in DCM (50 mL) and cooled to 0CC. Cyclopentanol (7.4 mL, 82 mmol), EDO (7.86 g, 41 mmol) and DMAP (0.33 g, 2.7 mmol) were then added and the reaction allowed to warm to RT, and stirred for 24 hrs. Water (100 mL) and DCM (50 mL) were then added and the layers separated. The aqueous layer was reextracted with DCM (2 x 50 mL) and the combined organic layers were then dried over Mg504 and concentrated in vacuo. Purification by column chromatography (40% EtOAc/heptane) afforded the title compound as a colourless oil (10.4 g, 88%). LCMS: m/z 455 [M+Na]., 149057-19-2

The synthetic route of 149057-19-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHROMA THERAPEUTICS LTD; DAVIES, Stephen John; PINTAT, Stephane; NORTH, Carl Leslie; MOFFAT, David Festus Charles; WO2014/1802; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics