Tag: M.W:200-300

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Into a 500 mL reaction flask, 200 mL of methanol was added to 25.0 g of methyl (3-chloro-3-phenylmethylene)-2-oxoindoline-6-formate oil which was obtained by rotary evaporation from the previous reaction step, stirred until fully dissolved, 20.9 g of compound VI and 15.5 g of diisopropylethylamine were added, heated to 50-60 C. and reacted for 10 hours until TLC showed the disappearance of the raw materials. The reaction solution was evaporated to dryness and replaced with 200 mL of ethyl acetate, washed with water (100 mL*3 times), and then 6.6 g of anhydrous magnesium sulfate was added for drying and 6.6 g of activated carbon was added for decolorization successively. The obtained solution was evaporated to dryness and replaced with methanol/n-heptane, crystallized to obtain 37.1 g of nintedanib, yield 86.1%. 1H NMR (400 MHz, DMSO-d6): 12.17 (s, 1H), 11.03 (s, 1H), 7.64-7.59 (t, J=7.6 Hz, 2H), 7.56-7.52 (t, J=7.6 Hz, 2H), 7.50-7.45 (d, J=7.6 Hz, 1H), 7.43-7.40 (d, J=1.6 Hz, 1H), 7.21-7.17 (d, J=8.3 Hz, 1H), 7.15-7.07 (m, 2H), 6.82-6.77 (m, 2H), 5.85-5.83 (d, J=8.3 Hz, 1H), 3.79 (s, 3H), 3.11-3.04 (m, 3H), 2.75-2.66 (m, 2H), 2.27-2.19 (m, 5H), 2.16-2.11 (m, 3H), 2.10 (s, 3H). Mass: 540.2 [M+H+]., 262368-30-9

The synthetic route of 262368-30-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Zhejiang Huahai Pharmaceutical Co., Ltd.; Shanghai Syncores Technologies, Inc.; Li, Zeng; Cheng, Xiaosong; He, Xianliang; Zhang, Jicheng; Huang, Luning; Tao, Anping; Gu, Hong; (14 pag.)US2020/48225; (2020); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5521-39-1,2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol,as a common compound, the synthetic route is as follows.,5521-39-1

Synthesis of //ONo.is-4-(5-Bromo-2-{4-[4-(2- hydroxy-ethyl)-piperazin-l-yl]-phenylamino}-pyrimidin-4-ylamino)adamantan-l-ol:Conc.HCl (20mL) was added to a mixture of tra?s-4-(5-bromo-2-chloropyrirnidin-4- ylamino)adamantan-l-ol (50mg, 139 mmoles) and 2-[4-(4-aminophenyl)piperazin-l- yl]ethanol (37mg, 0.167mmoles) in n-butanol (3ml) was and the mixture was heated at 1 10- 120 overnight. The reaction mixture was cooled to 80, n-butanol (5 ml) was added and filtered. The residue was triturated with hot MeOH, purified by preparative HPLC to afford lOmg of trara-4-(5-Bromo-2-{4-[4-(2-hydroxy-ethyl)-piperazin-l-yl]-phenylamino}- pyrimidin-4-ylamino)adamantan-l-ol inl3% yield.’H NMR (DMSO-d6) delta 10.2-10.35 (br s, H), 9.2-9.3 (br s,lH), 8.1-8.2 (s,lH), 7.5 (d,2H), 7.0 (d,2H)?6.2(s,lH), 3.0-4.0 (m,12H), 2.2-2.3 (s,2H), 2.0-2.1 (s,lH), 1.6-1.8 (m,7H), 1.3-1.5 (m,4H) LC-MS: 543 (M + l)

The synthetic route of 5521-39-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AURIGENE DISCOVERY TECHNOLOGIES LIMITED; SENGUPTA, Saumitra; RAJAGOPALAN, Srinivasan; BELAVAGI, Ningaraddi; RAMACHANDRA, Muralidhara; WO2012/59932; (2012); A1;,
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78818-15-2, Benzyl 3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,78818-15-2

EXAMPLE A; Preparation of Compound A of Formula 1 Process for the Preparation of Compound A-In-2:[00118] This compound was prepared by the method described by Bryant, HJ. et al, in WO 01/44250.[00119] To a stirred and cold (ice-bath cooling) suspension of benzyl 3- oxopiperazine-1-carboxylate (A-In-I) (1.00 g) and K2CO3 (11.8 g) in CH2Cl2 (40 mL) was added under N2 trimethyloxonium tetrafluoroborate (2.20 g, from Aldrich) in one portion. The cooling bath was removed and the mixture was stirred at room temperature under N2 for 19 h. This mixture was poured into water (40 mL) under ice-cooling and the organic phase was collected. The aqueous phase was extracted with CH2Cl2. The combined CH2Cl2 phases were washed with water (20 mL), then with brine, dried (Na2SO4) and concentrated. The crude residual oil was purified by silica gel column chromatography (5% MeOH/CH2Cl2) to give the title compound A- In-2 as colorless oil.

The synthetic route of 78818-15-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; WO2009/158394; (2009); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

129779-30-2, To a solution of tert-butyl czs-3,5-dimethylpiperazine-l-carboxylate (1.80 g, 8.40 mmol) in DCM (20 mL) was added a 37% HCHO solution (0.34 mL, 12.0 mmol) dropwise at 0 C, followed by portion- wise addition of Na(OAc)3BH (2.31 g, 10.9 mmol). The reaction mixture was stirred at room temperature for 4 h. The reaction mixture was diluted with DCM (30 mL) and washed with NaHC03 (20 mL) solution. The organic layer was separated, washed with brine (20 mL), dried over anhydrous Na2S04 and concentrated in vacuo to afford tert-butyl czs-3,4,5- trimethylpiperazine-l-carboxylate (1.81 g crude) as a colorless liquid. This compound was used as such for the next reaction without further purification. LC/MS (ESI) m/e [M+H]+/RT (min)/%: 228.90/4.29/88.5%. 1H NMR (400 MHz, CDC13) delta 1.08 (d, J = 6.1 Hz, 6H), 1.48 (s, 9H), 2.04-2.18 (m, 2H), 2.26 (s, 3H), 2.56-2.62 (m, 2H), 3.78-3.98 (m, 2H).

129779-30-2 (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 10822535, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NEUROPORE THERAPIES, INC.; WRASIDLO, Wolfgang; STOCKING, Emily, M.; HALL, Adrian; MACCOSS, Malcolm; (139 pag.)WO2017/20010; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: A mixture of 4-chloro-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine 12 (1 g, 4.34 mmol) and 1,4-dioxa-8-azaspiro[4.5]decane (0.62 g, 4.34 mmol) in 2-propanol (30 mL) or 95% ethanol for other amines was refluxed for two hour. The white solid formed in the hot solution was collected after cooling and further recrystallized from ethanol yielded white crystals of compound 13a (67%), 30459-17-7

As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference£º
Article; Abdelazeem, Ahmed H.; Abdelatef, Shaimaa A.; El-Saadi, Mohammed T.; Omar, Hany A.; Khan, Shabana I.; McCurdy, Christopher R.; El-Moghazy, Samir M.; European Journal of Pharmaceutical Sciences; vol. 62; (2014); p. 197 – 211;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13349-91-2,1-(2,2,2-Trifluoroethyl)piperazine dihydrochloride,as a common compound, the synthetic route is as follows.

General procedure: To a stirred suspension of 5-chloro-2-[[5-methyl-3-(6-methyl-3-pyridyl)isoxazol-4- yl]methyl]pyridazin-3-one (building block A, 300 mg, 0.947 mmol) and (R)-3- hydroxypyrrolidine (0.14 mL, 1.73 mmol) in DMSO (0.5 mL) and acetonitrile (3 mL) was added potassium carbonate (393 mg, 2.84 mmol) Then the reaction mixture was stirred at 70 C for 18 h. After cooling to room temperature the reaction mixture was diluted with EtOAc (80 mL) was washed three times with water (10 mL) and brine (10 mL). The aqueous layers were back extracted twice with EtOAc (80 mL). The combined organic extracts were dried (Na2S04), filtered and concentrated in vacuo. Purification by flash chromatography (silica, gradient: 0% to 10% MeOH in CH2CI2) afforded the title compound (341 mg, 93 %) as an off-white foam. MS (ESI): 368.2 ([M+H]+).

13349-91-2, 13349-91-2 1-(2,2,2-Trifluoroethyl)piperazine dihydrochloride 16312067, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CECERE, Giuseppe; GROEBKE ZBINDEN, Katrin; HERNANDEZ, Maria-Clemencia; KNUST, Henner; KOBLET, Andreas; OLIVARES MORALES, Andres Miguel; PATINY-ADAM, Angelique; PINARD, Emmanuel; RUNTZ-SCHMITT, Valerie; STEINER, Sandra; (328 pag.)WO2019/238633; (2019); A1;,
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692058-21-2, 1-Boc-4-(2,2,2-trifluoroethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,692058-21-2

tert-butyl 4-(2,2,2-trifluoroethyl)piperazine-1-carboxylate (253 mg, 0.94 mmol) was dissolve in DCM (9 mL) and a solution of 4 M HCI in dioxane (4.72 mL, 18.9 mmol) was added. The reaction was stirred 3 h at rt. The product was then concentrated in vacuum and co evaporated with DCM 3 times, affording the title compound (200 mg, 0.977 mmol, 100%) as beige solid.

As the paragraph descriping shows that 692058-21-2 is playing an increasingly important role.

Reference£º
Patent; BANTAM PHARMACEUTICAL, LLC; SIDDIQUI, Arshad, M.; CIBLAT, Stephane; DERY, Martin; CONSTANTINEUA-FORGET, Lea; GRAND-MAITRE, Chantal; BRUNEAU-LATOUR, Nicolas; SHIPPS, Gerald, W.; COOPER, Alan, B.; OZA, Vibha; KOSTURA, Matthew, W.; LUTHER, Michael; LEVINE, Jedd; (174 pag.)WO2018/102453; (2018); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.859518-35-7,tert-Butyl 3-cyanopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

859518-35-7, Step C tert-Butyl 3-cyano-4-(2-(2-hydroxyethoxy)ethyl)piperazine-1-carboxylate A solution of tert-butyl 3-cyanopiperazine-1-carboxylate, prepared as described in the previous step, (10 g, 0.047 mol) and 2-(2-hydroxyethoxy)acetaldehyde (14.8 g) (see: Bodin, A., Contact Dermatitis, 2001, 44:207) in dichloromethane was treated with formic acid (12.7 g), and the reaction mixture was stirred at room temperature overnight. Sodium cyanoborohydride (7.2 g, 0.118 mol) was added in portions. The reaction mixture was stirred at room temperature for 3 hours followed by the addition of water and extraction with dichloromethane. The organic layer was washed with brine, dried over sodium sulfate, filtered, and concentrated. The crude product was purified by column chromatography to provide the product. 1H NMR: (CDCl3, 400 MHz): delta (ppm) 4.15 (s, 1H), 3.69-3.63 (m, 4H), 3.58 (d, J=4.4 Hz, 2H), 3.47-3.44 (m, 4H), 2.61 (d, J=5.2 Hz, 2H), 2.51-2.48 (m, 4H), 1.43 (s, 9H).

859518-35-7 tert-Butyl 3-cyanopiperazine-1-carboxylate 53487922, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Hryhorenko, Eric; Sankaran, Banumathi; DeCory, Thomas R.; Tubbs, Theresa; Colt, Linda; Remmerie, Bart M.; Salter, Rhys; Donahue, Matthew Garrett; Gong, Yong; US2014/57305; (2014); A1;,
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259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 7-bromo-5-chloro-furo[3,2-b]pyridine-2-carboxylic acid (200 mg, 0.723 mmol) and tert-butyl 3,3-dimethylpiperazine-1-carboxylate (164.3 mg, 0.767 mmol) in DMF (2.13 mL) was added N-methyl morpholine (329.2 mg, 357.8 muL, 3.26 mmol) at ambient temperature. T3P (575.4 mg, 0.904 mmol) 50% W/W in DMF was added dropwise and the solution was stirred at room temperature for 30 minutes. NaHCO3 was added and the aqueous phase was extracted with EtOAc 3 times. The combined organic phase was washed with sat aq. ammonium chloride and brine, dried over MgSO4, filtered and evaporated under reduced pressure. The residue was purified by silica gel chromatography affording the title compound, tert-butyl 4-(7-bromo-5-chloro-furo[3,2- b]pyridine-2-carbonyl)-3,3-dimethyl-piperazine-1-carboxylate (295 mg, 0.6240 mmol, 86.26%). ESI-MS m/z calc.471.05606, found 472.24 (M+1)+; Rt: 2.05 min using Method C

259808-67-8, 259808-67-8 1-Boc-3,3-Dimethylpiperazine 22710387, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; SAYEGH, Camil Elie; STURINO, Claudio; FOURNIER, Pierre-Andre; LACOSTE, Jean-Eric; DIETRICH, Evelyne; MARTEL, Julien; VALLEE, Frederic; (494 pag.)WO2016/154075; (2016); A1;,
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53788-49-1, tert-Butyl 4-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,53788-49-1

t-BOC-Protected methylpiperizine was heated in the presence of l-fluoro-4- nitrobenzene under pressure in benzene to give 4-t-BOC-protected 1-methyl-1- (4- nitrophenyl) piperazinium salt. The piperazinium salt was heated in the presence of potassium [F] fluoride and Krytofix at 200C for 10 minutes. The oil was treated with aq. 3 M HC1 for 20 minutes to give [F-18]-1-methyl-1-(4-fluorophenyl) piperazinium chloride

53788-49-1 tert-Butyl 4-methylpiperazine-1-carboxylate 11401394, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; THE GENERAL HOSPITAL CORPORATION; WO2005/82425; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics