Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The product from example 69 part d) (1 g), the product from example 13 part b) (1.263 s g) and MgSO4 (xs) were stirred in THF (50 ml) for 16 h. Sodium triacetoxy borohydride (3.96 g) was added and the reaction stirred for 16 h. The reaction was quenched with water and extracted with ethyl acetate. The organic layer was dried (Na2SO4) and concentrated in vacuo. It was purified by chromatography (silica, (20percent EtOAc/isohexane as eluent)), to give the sub-titled compound as a colourless oil (2.03 g). o MS: APCI (+ve): 469 (M+l), 325145-35-5

The synthetic route of 325145-35-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/56752; (2006); 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.475272-54-9,(S)-1-Boc-3-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

2-Amino-4,6-dichloropyrimidine-5-carbaldehyde (2.4 g, 13 mmol) and tert-butyl (35)-3-isopropylpiperazine-l -carboxylate (2.9 g, 13 mmol) in 1,4-dioxane (50 mL) were treated with DIPEA (3.3 g, 5 mL, 25 mmol) and heated at 90C for 6 h. The reaction mixture was cooled and concentrated in vacuo, then partitioned between DCM and water. The organic layers were phase separated and concentrated. The resulting golden foam was taken up in THF (100 mL) with triethylamine (2.7 g, 4 mL, 27 mmol) and methylhydrazine (0.64 g, 0.73 mL, 14 mmol), then stirred for 72 h at room temperature. The reaction mixture was concentrated in vacuo and partitioned between DCM and water, then phase separated. The organic layers were further concentrated in vacuo. The residual foam was taken up in DCM (100 mL), then 4N HC1 in 1,4-dioxane (20 mL) was added and the mixture was stirred overnight. The resultant solution was concentrated in vacuo and triturated with diethyl ether to give the title compound (3.8 g, 95%) as a sticky foam that was >95% pure by LCMS. LCMS (ES+) [M+H]+ 276.2, RT 0.72 minutes (method 2).

475272-54-9, 475272-54-9 (S)-1-Boc-3-Isopropylpiperazine 24820348, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; UCB PHARMA S.A.; KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D; FORD, Daniel James; FRANKLIN, Richard Jeremy; GHAWALKAR, Anant Ramrao; HORSLEY, Helen Tracey; HUANG, Qiuya; REUBERSON, James Thomas; VANDERHOYDONCK, Bart; WO2014/96423; (2014); A1;,
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Piperazines – an overview | ScienceDirect Topics

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.

[21851 Step 1: Synthesis of tert-butyl(3R.5S?)-4-(3-formylbenzyl)-3 .5-dimethylpiperazine- 1 -carboxylate[21861 (3R,55)-tert-butyl 3 ,5-dimethylpiperazine- 1 -carboxylate (formula 8-1, 2.730 g, 12.739 mmol), 3-(bromomethyl)benzaldehyde (2.789 g, 14.013 mmol) and Cs2CO3 (8.301 g, 25.478 mmol) were mixed in acetonitrile (50 mL) at room temperature, and the mixture was stirred at the same temperature for 18 hours. The reaction mixture was filtered through a paper filter to remove solids, and the filtrate was purified by column chromatography (silicon dioxide, 120 g cartridge; ethyl acetate/hexane = from 5 % to 30 %) and concentrated to afford the desired compound (2.730 g, 64.5 %) as a yellow oil.

129779-30-2, The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; SONG, Hyeseung; LEE, Changgon; KWAK, Dalyong; LEE, Jaeyoung; BAE, Suyeal; KIM, Yuntae; BAE, Daekwon; HA, Nina; BAE, Miseon; KIM, Jihyun; WO2015/137750; (2015); A1;,
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Piperazines – an overview | ScienceDirect Topics

31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In 2 mL of dimethyl acetamide were combined tert-butyl 4-chloro-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxylate (1.0 g, 3.7 mmol), triethylamine (1.0 mL, 7.4 mmol), and benzyl 1-piperazinecarboxylate (0.86 mL, 4.4 mmol). The reaction vessel was sealed and the reaction mixture was heated to 90¡ã C. with stirring. After 5 hours, the reaction was diluted with brine and extracted with methyl t-butyl ether. The combined organic layers were washed sequentially with saturated ammonium chloride and brine, dried over MgSO 4, and concentrated under reduced pressure to a thick oil. The oil was chromatographed (RediSep , 24 g) eluting with 1:1 ethyl acetate/Hexanes to give tert-butyl 4-(4-((benzyloxy)carbonyl)piperazin-1-yl)-5,8-dihydropyrido [3,4-d]pyrimidine-7(6H)-carboxylate (1.3 g, 2.9 mmol, 77% yield). ES+APCI MS m/z 454.2 [M+H] +., 31166-44-6

As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference£º
Patent; Mirati Therapeutics, Inc.; Array BioPharma Inc.; Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Cook, Adam; Fell, Jay Bradford; Fischer, John P.; Marx, Matthew Arnold; Mejia, Macedonio J.; Savechenkov, Pavel; Vigers, Guy P.A.; Smith, Christopher Ronald; Rodriguez, Martha E.; US2019/144444; (2019); A1;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Tert-butyl (S)-3-(hydroxymethyl)piperazine-1-carboxylate (887 mg, 4.1 mmol) was added to 53 7-bromo-4,6-dichloro-3-nitroquinoline (600 mg, 1.86 mmol), and 56 DIPEA (0.664 ml, 3.73 mmol) in NMP (4.5 ml) in a microwave tube, which was sealed and heated at 80 C. in a microwave reactor for 60 mins. To the reaction mixture was added 63 DCM (150 ml), and the organic layer was washed with water (3¡Á100 ml), brine, dried and evaporated to give a crude residue. The crude product was purified by flash silica chromatography, elution gradient 10 to 30% 57 EtOAc in 58 heptane. Pure fractions were evaporated to dryness to afford 91 tert-butyl (S)-4-(7-bromo-6-chloro-3-nitroquinolin-4-yl)-3-(hydroxymethyl) piperazine-1-carboxylate (365 mg, 39%) as a yellow solid. 1H NMR (500 MHz, DMSO, 27 C.) 1.44 (9H, s), 3.43-3.48 (2H, m), 3.76 (1H, s), 3.85-3.9 (1H, m), 3.96-4.05 (1H, m), 4.07-4.31 (3H, m), 4.58 (1H, t), 8.38 (1H, s), 8.50 (1H, s), 9.05 (1H, s), 11.15 (1H, s). m/z: ES+ [M+H]+ 501, 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 15 Preparation of (2S)-(-)-1-(4-indolyloxy)-3-(4-(4-trifluoromethylphenyl)piperazin-1-yl)-2-propanol ethanedioate The title compound was prepared in similar fashion from (S)-(+)-4-(oxiranylmethoxy)-1H-indole and 1-(4-trifluoromethylphenyl)piperazine. The resulting free base was dissolved in ethyl acetate, and precipitated with one equivalent of oxalic acid in ethyl acetate in 89% overall yield. FDMS m/e=419 (M+ of free base)., 30459-17-7

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

Reference£º
Patent; Eli Lilly Company; US5789402; (1998); A;,
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Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1 ,1-dimethylethyl (3R)-3-methyl-1-piperazinecarboxylate (301 mg, 1.5 mmol) in anhydrous acetonitrile (1OmL) was added PS-DIEA (925mg) and the solution was stirred gently under an argon atmosphere at room temperature for 15mins. 4-chlorobenzenesulfonyl chloride (371 mg, 1.8 mmol) as a solution in acetonitrile (5ml_) was added and the reaction was stirred for 24hrs. After this time, the reaction was filtered and PS-isocyanate (3g) was added to the solution which was stirred at room temperature over a weekend (approx 64hrs). The reaction was again filtered and PS-trisamine (1.2g) was added to the solution mixture which was stirred for 2hrs at room temperature. Finally the reaction was filtered and reduced in- vacuo to yield the title compound (411 mg, 73%).1H-NMR (CDCI3) 51.02 (3H, d, J= 6.8Hz), 1.43 (9H, s), 2.79 (1 H, br m), 2.97 (1 H, br m), 3.11 (1 H, dt J=12.5, 3.29Hz), 3.60 (1 H, m), 3.80 (1 H, br m), 4.1 1 (2H, br m), 7.48 (2H, m), 7.75 (2H, m)

163765-44-4, 163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXO GROUP LIMITED; BESWICK, Paul, John; CAMPBELL, Alister; CRIDLAND, Andrew; GLEAVE, Robert, James; PAGE, Lee, William; WO2010/102663; (2010); 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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

Preparation of 1-tert-butyl 3-methyl 4-(4′-chloro-2′-fluoro-4-nitrobiphenyl-3-carbonyl)piperazine-1,3-dicarboxylate (6)Starting material 5 (708 mg, 2.9 mmol) in 20 ml of dichloromethane is initially introduced in a 50 ml multinecked flask with dropping funnel, thermometer and N2 inlet lube, and 1.7 ml of DIPEA are added. The solution is cooled to 0 C., and a solution of 900 mg (3 mmol) of starting material 4 in 10 ml of dichloro-methane is added dropwise over the course of 15 min with stirring. The ice bath is then removed, and the mixture is stirred for a further one hour. Water is added to the reaction mixture, the organic phase is separated off, dried over sodium sulfate, and the solvent is removed. The residue is filtered absorptively through a silica-gel column with ethyl acetate, and the filtrate is evaporated to dryness. The desired product 6 is obtained in a yield of 80% (1.5 g, 2.3 mmol) as solid (mass: [M*-(tBu)]=266; RT 3.44 min. HPLC method 1-100-2_Speed).

129799-08-2, As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference£º
Patent; Merck Patent Gesellschaft Mit Beschrankter Haftung; US2012/115852; (2012); 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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of 10 (100 mg, 0.33 mmol) and 1-(4-trifluoromethylphenyl)piperazine (85 mg,0.37 mmol) in DMF (0.5 mL) was added solid K2CO3 (82 mg, 0.59 mmol). The resulting suspensionwas stirred at 90 C for 48 h. Water (5 mL) and DCM (5 mL) were added and the phases were separated.The aqueous phase was then extracted with further DCM (2 5 mL). The organics were dried over anh.Na2SO4, filtered and evaporated in vacuo to give a yellowish solid (161 mg). Column chromatography(hexane/EtOAc mixture) gave 15 as a white solid (52 mg, 32% yield). The analytical sample wasobtained by washing with cooled pentane (38 mg), m.p. 157-158 C. IR (ATR) : 667, 711, 721, 744,770, 806, 824, 909, 951, 971, 984, 1039, 1070, 1106, 1157, 1199, 1230, 1330, 1354, 1390, 1429, 1493, 1522,1594, 1615, 2847, 2919 cm1. 1H-NMR (400 MHz, CDCl3) : 0.10-0.18 (complex signal, 2H, 9-H2),0.84-0.98 (complex signal, 2H, 8-H and 10-H), 2.54-2.66 (complex signal, 2H, 2-H and 6-H), 2.75 (m, 1H,1-H or 7-H), 2.90 (m, 1H, 7-H or 1-H), 3.26 (m, 1H, 3-Ha or 5-Ha), 3.41 [t, J = 5.4 Hz, 4H, 2?(6?)-H2],3.48 (m, 1H, 5-Ha or 3-Ha), 3.56-3.82 [complex signal, 6H, 3-Hb, 5-Hb, 3?(5?)-H2], 5.69 (m, 1H, 11-Hor 12-H), 5.85 (m, 1H, 12-H or 11-H), 6.65 (d, J = 8.8 Hz, 1H, 50-H), 6.95 [d, J = 8.6 Hz, 2H, 2??(6??)-H],7.50 [d, J = 8.6 Hz, 2H, 3??(5??)-H], 7.66 (dd, J = 8.8 Hz, J? = 2.2 Hz, 1H, 40-H), 8.31 (d, J = 2.2 Hz, 1H,20-H). 13C-NMR (100.5 MHz, CDCl3) : 3.9 (CH2, C9), 10.2 (broad s, CH, C8 and C10), 35.6 (CH, C1and C7), 42.7 (CH, C2 or C6), 44.5 [CH2, C3?(5?)], 45.1 (CH, C6 or C2), 47.7 [CH2, C2?(6?)], 49.6 (CH2,C3 or C5), 53.6 (CH2, C5 or C3), 105.8 (CH, C50), 114.6 [CH, C2??(6??)], 120.8 (q, J = 32 Hz, C, C4??),122.1 (C, C30), 124.6 (q, J = 269 Hz, C, CF3), 126.4 [q, J = 4 Hz, CH, C3??(5??)], 128.1 (CH, C11 or C12),129.3 (CH, C12 or C11), 137.5 (CH, C40), 147.5 (CH, C20), 153.0 (C, C1??), 159.1 (C, C60), 167.0 (C, CO).HRMS-ESI + m/z [M + H]+ calcd. for [C28H29F3N4O + H]+: 495.2396, found: 495.23692.

30459-17-7, The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Leiva, Rosana; McBride, Andrew; Binnie, Margaret; Webster, Scott P.; Vazquez, Santiago; Molecules; vol. 23; 3; (2018);,
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.303-26-4,1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

Example 1 10 gr. (0.035 mole) of 1-[(4-chlorophenyl)phenylmethyl]piperazine, 8.8 gr. (0.0525 mole) of ethyl 2-chloroethoxyacetate and 50 ml. of triethylamine were introduced into a pressure vessel. The mixture was stirred at 135 C. for 10 hours. It was cooled to 20 C. and filtered. The filtrate was evaporated and then distilled at 10 mbar pressure in order to remove the excess of the unreacted ethyl 2-chloroethoxyacetate. The oily residue obtained is sufficiently pure for the preparation of cetrizine by hydrolysis. The residue was purified over a silica gel chromatographic column. 13 gr. of ethyl [2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetate is obtained as dark red oil (89.4% yield).

303-26-4, As the paragraph descriping shows that 303-26-4 is playing an increasingly important role.

Reference£º
Patent; Chemiagis, Ltd.; US6100400; (2000); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics