Tag: M.W:200-300

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The (2i?,65)-l-(iV-benzyloxycarbonylglycyl)-2,6-dimethylpiperazine used as a starting material was prepared as follows :-; Diisopropylethylamine (0.4 ml) was added to a stirred mixture of ter t-butyl (3i?,55)-3,5-dimethylpiperazine-l-carboxylate (0.25 g; available from Atlantic SciTech Group, Inc., 601 East Linden Avenue, Linden, New Jersey 07036, USA)), N- benzyloxycarbonylglycine (0.296 g), 2-(7-azabenzotriazol-l-yl)-l,l,3,3-tetramethyluronium hexafluorophosphate (V) (0.555 g) and DMA (15 ml) and the resultant mixture was stirred at ambient temperature for 18 hours. The reaction mixture was evaporated and the residue was dissolved in a mixture of trifluoroacetic acid (1.5 ml) and methylene chloride (4.5 ml). The mixture was stirred at ambient temperature for 1 hour. The resultant mixture was evaporated. Methanol was added to the residue and the solution was loaded onto an Isolute SCX-2 cation exchange cartridge (20 g). The column was washed with methanol and the product was eluted using a 3M methanolic ammonia solution. There was thus obtained (2i?,6.S)-l-(N-benzyloxycarbonylglycyl)-2,6-dimethylpiperazine (0.46 g); Mass Spectrum: M+H+ 306; HPLC: method Bl, Retention Time 2.37 minutes.

129779-30-2, As the paragraph descriping shows that 129779-30-2 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2008/32064; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5747-48-8, Preparation BA toluene solution of 1 l-piperazin-l-yldibenzo[b,fj[l,4]thiazepine (1500 mL, 0.686 mol) prepared by reaction of piperazine with 1 l-chloro-dibenzo[b,fj[l,4]-thiazepine in toluene (see, e.g., U. S. Pat. No. 4,879,288) was treated with 1500 mL deionized water and 90 mL of HCl (32% w/w). The resulting mixture was heated to 70 0C and agitated for 45 min. Agitation was ceased and the mixture allowed to settle and phase separate for 30 min. The lower aqueous phase, containing the HCl salt of 1 l-piperazin-l-yldibenzo[b,fj[l54]thiazepine was isolated. The aqueous phase was then treated with 1000 mL of toluene and 99 g of aqueous NaOH (47% w/w). The resulting mixture was heated to 70 C and agitated for 45 EPO min. Agitation was ceased and the mixture allowed to settle and phase separate for 30 min. The lower aqueous phase was discarded and the upper organic phase retained to which 300 mL of deionized water was added. The resulting mixture was agitated for 15 min and then allowed to settle for 30 min. The aqueous phase was discarded and the organic phase retained. The organic phase was extracted once more with 300 mL of deionized water. About 750 mL of toluene from the organic phase was distilled out. The resulting concentrate was cooled to 60 C, then 200 mL of methyl-t-butyl ether (MTBE) was added. The resulting mixture was cooled to ambient temperature then seeded with Form A seed crystals. The seeded mixture was then cooled to 10 C and held at this temperature for 3 hours under slow agitation. The resulting solid was isolated under suction via a no. 3 sinter. The solid product was then washed with 120 mL of MTBE at ambient temperature and dried at 40 C under vacuum resulting in 175 g (86.4%) of crystalline product. Assay 99.9% w/w by HPLC area %.

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; WO2006/73360; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of tert-butyl 4-(2-((3-cyano-4-(6-(4-(5-fluoro-2- methylbenzamido)-4-methylpiperidin-l-yl)pyridin-3-yl)pyrazolo[l,5-a]pyridin-6- yl)oxy)ethyl)piperazine-l-carboxylate. To a mixture of N-(l-(5-(3-cyano-6- hydroxypyrazolo[l,5-a]pyridin-4-yl)pyridin-2-yl)-4-methylpiperidin-4-yl)-5-fluoro-2- methylbenzamide (Intermediate P68; 55 mg, 0.114 mmol), tert-Butyl 4-(2- chloroethyl)tetrahydro-l(2H)-pyrazine carboxylate (57 mg, 0.227 mmol) was added cesium carbonate (148 mg, 0.454 mmol) in DMA (1 mL) and was stirred overnight at 60C. After cooling to ambient temperature, reaction was diluted with EtOAc and washed with water and the organic extracts were dried over anhydrous Na2S04(S), filtered and concentrated in vacuo. The residue was purified using silica chromatography (50-100%) EtOAc in Hexanes) to afford the title compound (49 mg, 62% yield) MS (apci) m/z=697.4 (M+H).

208167-83-3, 208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ANDREWS, Steven W.; ARONOW, Sean; BLAKE, James F.; BRANDHUBER, Barbara J.; COLLIER, James; COOK, Adam; HAAS, Julia; JIANG, Yutong; KOLAKOWSKI, Gabrielle R.; MCFADDIN, Elizabeth A.; MCKENNEY, Megan L.; MCNULTY, Oren T.; METCALF, Andrew T.; MORENO, David A.; RAMANN, Ginelle A.; TANG, Tony P.; REN, Li; WALLS, Shane M.; (946 pag.)WO2018/71454; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

16154-72-6, 3-Chloro-4-(4-methylpiperazin-1-yl)benzenamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To obtain the title compound of Example 31 , 5-(2-chloro-4-pyrimidinyl)-lambda/-ethyl-4-[3- methyl-5-(methyloxy)phenyl]-1 ,3-thiazol-2-amine (0.066 g, 0.183 mmol), prepared by a procedure analogous to Example 25, Step F, and [3-chloro-4-(4-methyl-1- piperazinyl)phenyl]amine (0.041 g, 0.183 mmol) were combined with iPrOH (2 ml.) and concentrated HCI (2 drops) in a microwave vial. The reaction was heated to 18O0C for 20 min in the microwave then cooled to rt. TEA (approx. 0.1 ml.) and silica gel were combined with the reaction and the resulting mixture was concentrated to dryness and subsequently adhered to silica gel. Column chromatography using EtOAc, MeOH, and NH4OH yielded fractions which were concentrated to dryness. This material was then further purified on a reverse phase acidic HPLC. The resulting fractions were free-based via extraction and concentrated to dryness to yield 35 mg of the title compound of Example 31 (35%Y). 1H NMR (400 MHz,DMSO-d6) delta 9.51 (s, 1 H), 8.25 (t, J = 5.4 Hz, 1 H), 8.07 (d, J = 5.6 Hz, 1 H), 8.03 (d, J = 2.5 Hz, 1 H), 7.54 (dd, J = 8.8, 2.6 Hz, 1 H), 7.06 (d, J = 8.9 Hz, 1 H), 6.88 (s, 1 H), 6.82 (d, J = 9.7 Hz, 2 H), 6.29 (d, J = 5.5 Hz, 1 H), 3.72 (s, 3 H), 3.28 (m, 2 H), 2.91 (br, 4 H), 2.48 (m, 4 H), 2.30 (s, 3 H), 2.23 (s, 3 H), 1.19 (t, J = 7.0 Hz, 3 H). HRMS C28H33N7OSCI (M+H)+ calcd 550.2156, found 550.2167.

16154-72-6, The synthetic route of 16154-72-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SMITHKLINE BEECHAM CORPORATION; WO2009/32667; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

548762-66-9,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 4,4′-(chloromethylene)bis(fluorobenzene) (3.76 g, 15.75 mmol) in acetonitrile (15 mL) was added tert-butyl (2S,5R)-2,5-dimethylpiperazine-1-carboxylate (2.25 g, 10.50 mmol), followed by DIPEA (5.50 mL, 31.5 mmol). The reaction mixture was stirred at 85 C overnight. The reaction mixture was concentrated under reduced pressure to remove volatiles, the residue was dissolved in ethyl acetate (150 mL), and washed with water. The aqueous layer was back-extracted with ethyl acetate (100 mL x 2). The combined organic layer was washed with brine, dried over Na2SO4 and concentrated under reduced pressure to give the crude product, which was purified by silica gel chromatography on ISCO (5-10 % EtOAc/petroleum ether; 80 g column) to afford tert-butyl (2S,5R)-4-(bis(4-fluorophenyl)methyl)-2,5-dimethylpiperazine-1- carboxylate (3.55 g, 81 % yield). LCMS: m/z = 417.4 (M+H); rt 1.561 min. (LCMS Condition: Column: Kinetex XB-C18 (3 x 75 mm) 2.6 mm; Mobile phase A: 10 mM ammonium formate:acetonitrile (98:2), Mobile phase B: 10 mM ammonium (0508) formate:acetonitrile (2:98), Gradient = 20-100 % B over 4 minutes, then a 0.6 minute hold at 100 % B; Temperature: 27 C; Flow rate: 1.0 mL/min; Detection: UV at 220 nm).

As the paragraph descriping shows that 548762-66-9 is playing an increasingly important role.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; VELAPARTHI, Upender; CHUPAK, Louis S.; DARNE, Chetan Padmakar; DING, Min; GENTLES, Robert G.; HUANG, Yazhong; KAMBLE, Manjunatha Narayana Rao; MARTIN, Scott W.; MANNOORI, Raju; MCDONALD, Ivar M.; OLSON, Richard E.; RAHAMAN, Hasibur; JALAGAM, Prasada Rao; ROY, Saumya; TONUKUNURU, Gopikishan; VELAIAH, Sivasudar; WARRIER, Jayakumar Sankara; ZHENG, Xiaofan; TOKARSKI, John S.; DASGUPTA, Bireshwar; REDDY, Kotha Rathnakar; RAJA, Thiruvenkadam; (0 pag.)WO2020/6018; (2020); 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.

To a 50 mL of sealing tube were added 1-tert-butyl 3-methyl piperazine-1,3-dicarboxylate (500 mg, 2.05 mmol) , iodomethane (580mg, 4.10 mmol) , potassium carbonate (424 mg, 3.07 mmol) and acetone (10 mL) .The mixture was stirred at 50 for 6 h and concentrated. The residue was diluted withwater (20 mL) . The resulting mixture was extracted with DCM (10 mL ¡Á 3) . The combined organic layers were dried over anhydrous Na2SO4and concentrated to give 1-tert-butyl 3-methyl 4-methylpiperazine-1,3-dicarboxylate as a light yellow solid (290 mg, 54) . 1H NMR (400 MHz, CDCl3): delta ppm 4.65-4.83 (m, 1H) , 4.29-4.33 (m, 1H) , 4.18-4.23 (m, 1H) , 4.05-4.11(m, 1H) , 3.80-3.94 (m, 3H) , 3.88 (s, 3H) , 3.66 (s, 3H) , 1.48 (s, 9H) and MS-ESI: m/z 259.30 [M+H] +.

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

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (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.169447-86-3,(S)-tert-Butyl 2-benzylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 122 and 123 (-0.216 mmol) in dioxane (3 ml_) was added (S)~N-Boc-2-benzylpiperazine (0.07 g, 0.254 mmol) and diisopropylethylamine (0.077 ml_, 0.443 mmol). The reaction mixture was heated at 600C for 1 hour. The organic solvent was evaporated under reduced pressure. The crude product mixture was purified by RP-HPLC to yield 3-(3-methylindazol-5-yl)-5-[(S)-4-Boc-3-benzylpiperazin-1-yl]- [1 ,2,4]triazine 124 (0.012 g, 0.025 mmol) and 6-chloro-3-(3-methylindazol-5- yl) )-5-[(S)-4-Boc-3-benzylpiperazin-1-yl]-[1 ,2,4]triazine 125 (0.02 g, 0.038 mmol).

169447-86-3, The synthetic route of 169447-86-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SCHERING CORPORATION; WO2006/81230; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

To a solution of 100 mg (0.69 mmol) of 3-ethynyl benzoic acid in 5 mL of dry N,N-dimethylformamide, 164 mg (0.57 mmol) of 4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)aniline (prepared as described in J. Med. Chem., (2010) 53, 4701-4719) 242 mg (0.75 mmol) of TBTU and 0.14 mL (0.82 mmol) of DIPEA were added consecutively. After 15 h under stirring at room temperature the mixture was poured into aqueous NaHC03 and extracted twice with ethylacetate. The organic phase was then washed with brine, dried over Na2S04 and evaporated to dryness. A flash- chromatography on silica gel (DCM-MeOH-NH3 7N in methanol 9/1/0.04), afforded 149 mg of the title compound (63%). 1H NMR (600 MHz, DMSO-d6) delta ppm 0.99 (t, J=7.14 Hz, 3 H) 2.19 – 2.46 (m, 10 H) 3.57 (s, 3 H) 6.61 (br. s., 2 H) 7.60 (t, J=7.88 Hz, 1 H) 7.64 (d, J=2.20 Hz, 1 H) 7.72 (d, J=8.61 Hz, 1 H) 7.80 (dt, J=7.83, 1.21 Hz, 1 H) 7.91 – 7.98 (m, 1 H) 8.05 (dd, J=8.52, 1.92 Hz, 1 H) 8.12 (s, 1 H) 8.16 (t, J=1.47 Hz, 1 H) 8.21 (d, J=2.20 Hz, 1 H) 10.59 (s, 1 H) 12.08 (br. s., 1 H) HRMS (ESI) calcd for C29H28N7OF3 [M+H]+ 548.2380, found 548.2392.

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference£º
Patent; NERVIANO MEDICAL SCIENCES S.R.L.; ANGIOLINI, Mauro; BUFFA, Laura; MENICHINCHERI, Maria; MOTTO, Ilaria; POLUCCI, Paolo; TRAQUANDI, Gabriella; ZUCCOTTO, Fabio; WO2014/184069; (2014); 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.208167-83-3,tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Preparation of tert-butyl 4-(2-((3-cyano-4-(6-(4-methyl-4- (picolinamido)piperidin-l-yl)pyridin-3-yl)pyrazolo[l,5-a]pyridin-6-yl)oxy)ethyl)piperazine- 1-carboxylate. To a solution of N-(l-(5-(3-cyano-6-hydroxypyrazolo[l,5-a]pyridin-4- yl)pyridin-2-yl)-4-methylpiperidin-4-yl)picolinamide (Intermediate P90, 120 mg, 0.265 mmol) in DMA (2.646 mL) was added tert-Butyl 4-(2-chloroethyl)tetrahydro-l(2H)- pyrazinecarboxylate (65.8 mg, 0.265 mmol) and cesium carbonate (431 mg, 1.32 mmol). The reaction mixture was stirred at 60C for 48 h. After cooling to ambient temperature, the reaction mixture was diluted with 4: 1 DCM/IPA and washed successively with saturated NaHC03(aq) and saturated NaCl(aq). The organic extract was dried over anhydrous Na2S04(S), filtered, and concentrated in vacuo to afford the title compound (176 mg, 0.264 mmol, 99.9 % yield) in sufficient purity for step 2. MS (apci) m/z = 666.4 (M+H).

208167-83-3, The synthetic route of 208167-83-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ANDREWS, Steven W.; ARONOW, Sean; BLAKE, James F.; BRANDHUBER, Barbara J.; COLLIER, James; COOK, Adam; HAAS, Julia; JIANG, Yutong; KOLAKOWSKI, Gabrielle R.; MCFADDIN, Elizabeth A.; MCKENNEY, Megan L.; MCNULTY, Oren T.; METCALF, Andrew T.; MORENO, David A.; RAMANN, Ginelle A.; TANG, Tony P.; REN, Li; WALLS, Shane M.; (946 pag.)WO2018/71454; (2018); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: A Pyrex vessel was charged with magnetic stirring bar, (0.350 g, 2.00 mmol) of 2-methoxy-4-(oxiran-2-yl)benzonitrile, (0.457 g, 2.20 mmol) of tert-butyl (3S)-3-(hydroxymethyl)piperazine-1-carboxylate, and 6 mL of EtOH.Then it was introduced in the microwave reactor and irradiated at 150 C for 3 hr. Then the mixture was cooled toroom temperature and the solvent was evaporated and the resulting residue was purified by column chromatography(silica gel, 1- 20% dichloromethane/MeOH) which afforded the title compound as a mixture of two diastereomers(1:1). LC/MS: (IE, m/z) [(M + 1) – t-Bu]+ = 336.1., 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; Merck Sharp & Dohme Corp.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; (128 pag.)EP2744499; (2016); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics