Month: August 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

Levofloxacin carboxylic acid (225.0mg, 0.8mmol) was dissolved in DMSO (dimethyl sulfoxide, 5.0mL), was added TEA (triethanolamine, 0.44mL, 3.2mmol) and Compound S1-5 (259.5mg, 1.2mmol), at 90 deg.] C in a microwave reactor 24h. After completion of the reaction, cooled to room temperature, dichloromethane (15 mL), then washed three times (15 mL), dried over anhydrous yellow solid was recrystallized from ethanol to give 105.1 mg, yield 27.51% calculated measured

1030377-21-9 (S)-1-Boc-2-(Hydroxymethyl)piperazine 22884145, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; Guangdong Zhong Hospital; Guangdong Experiment Animal Monitor Suo; Liu Bo; Xu Guangyu; Yu Jie; Wu Yue; Chen Cha; Xu Fangfang; Zhang Yu; Han Xiaodong; Lin Dongling; Huang Ren; Lu Jinjian; Zhang Yuqin; (62 pag.)CN106674254; (2017); A;,
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31321-68-3, (R)-Piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The Boc protecting group of previous compound was removed at room temperature for one hour with a solution of AcOEt/HCl 4M. The mixture was then concentrated in vacuo, diluted with MeOH and concentrated several times in vacuo. The residue was then coupled with the corresponding acid (1.1 eq.), in the presence of BOP (1.1 eq.) and NMM (2.2 eq.) for two hours, in DCM. The mixture was then concentrated in vacuo and the residue dissolved in AcOEt. The organic layer was successively washed with aqueous solutions of 1M KHSO4, saturated NaHCO3 and brine. The organic layer was then dried over Na2SO4, filtered and concentrated in vacuo to yield the desired compound which was then treated with 4M AcOEt/HCl as already described if necessary. The final compound purified by preparative HPLC on a C18 column using a water/acetonitrile/TFA 0.1% gradient (yield around 50% for the three steps).

31321-68-3 (R)-Piperazine-2-carboxylic acid 6558437, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; AETERNA ZENTARIS GmbH; CENTRE NAT DE LA RECHERCHE SCIENTIFIQUE; University of Montpellier I; University of Montpellier II; US2009/239877; (2009); A1;,
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Piperazines – an overview | ScienceDirect Topics

59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (S) – 4 – (2-hydroxy-1-phenyl-ethylamine) – 5-methyl-pyrrolo [2,1-f] [1, 2, 4] triazine-6-carboxylic acid (100 mg, 0 . 32mmol) and 1-cyclopropanecarboxylic formyl piperazine (74 mg, 0 . 48mmol) dissolved in N, N-dimethyl formamide (8 ml) in, then add 1-hydroxy benzotriazole (52 mg, 0 . 39mmol), 1-ethyl-3 – (3-dimethylamino-propyl) carbodiimide hydrochloride (74 mg, 0 . 39mmol) and triethylamine (98 mg, 0 . 96mmol), stirring the mixture at room temperature until the TLC reaction monitoring raw material the reaction is complete, to be added in to the reaction solution (100 ml), ethyl acetate (50 ml ¡Á 3) extraction, then by saturated sodium chloride solution (100 ml ¡Á 2) washing, the organic phase is dried with anhydrous sodium sulfate, concentrated under reduced pressure, the resulting residue is purified with silica gel column chromatography, to obtain (S) – (4-cyclopropyl carbonyl-piperazine-1-yl) – [4 – (2-hydroxy-1-phenyl-ethylamine) – 5-methyl-pyrrolo [2,1-f] [1, 2, 4] triazin-6-yl]-methyl ketone (99 mg, white solid), yield: 69.0%.

59878-57-8 1-(Cyclopropylcarbonyl)piperazine 2064235, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; SHANGHAI CDYMAX PHARMACEUTICALS CO LTD; An, XiaoXia; Bie, PingYan; Yang, wuli; Liu, Jun; (49 pag.)CN103848833; (2016); B;,
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109384-27-2, 1-Methylpiperazin-2-one hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of ethyl 2-(4-methyl-3-oxopiperazin-l-yl)-2- phenylacetate (150). DIPEA (0.52 ml, 2.96 mmol) and l -methylpiperazin-2-one hydrochloride (0.22 g, 1.48 mmol) were sequentially added to a solution of ethyl 2-bromo-2-phenylacetate (0.22 ml, 1.23 mmol) in acetonitrile (4 ml). The reaction was stirred at room temperature for 1.5 hours. DIPEA (0.13 ml, 0.74 mmol) was added again and the reaction was stirred at room temperature overnight. The solvent was evaporated and the crude was purified by flash chromatography (DCM/Acetone = 9/1) to obtain ethyl 2-(4-methyl-3-oxopiperazin- l-yl)-2-phenylacetate (256 mg, 75 % yield) as a yellow oil. 1H NMR (300 MHz, DMSO-d6) ppm 6.91 – 7.66 (m, 5 H), 4.28 (s, 1 H), 3.99 – 4.22 (m, 2 H), 3.23 (t, 2 H), 3.00 (s, 2 H), 2.80 (s, 3 H), 2.61 – 2.71 (m, 2 H), 1.14 (t, 3 H).

As the paragraph descriping shows that 109384-27-2 is playing an increasingly important role.

Reference£º
Patent; CHIESI FARMACEUTICI S.P.A.; AMARI, Gabriele; PESENTI, Cristina; BOSSOLO, Stefano; WO2013/98145; (2013); A1;,
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129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 1 -benzhydrylazetidin-3-yl methanesulfonate (2.4 g, 7.56mmol), tert-butyl methyl piperazine-1,3-dicarboxylate (1.85 g, 7.56 mmol), K2C03 (1.6 g, 11.34 mmol) in CH3CN (40 mL)was stirred atreflux for 16 h. The mixture was partitioned between ethyl acetate and water. The organic layer was washed with waterand brine, dried over Na2504, and concentrated in vacuo. The residue was purified by flash column chromatography on silica gel (10% petroleum ether/ethyl acetate) to afford the desired product (1.85 g, 51% yield).

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; ARAXES PHARMA LLC; JANES, Matthew, Robert; PATRICELLI, Matthew, Peter; LI, Liansheng; REN, Pingda; LIU, Yi; (397 pag.)WO2016/44772; (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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

Intermediate 594-{2-[5-Chloro-2-(4-methanesulfonyl-piperazin-1 -yl)-pyrimidin-4-yl1-1 -hvdroxy-ethyl)- piperidine-1 -carboxylic acid tert-butyl esterA mixture of 4-[2-(2,5-dichloro-pyrimidin-4-yl)-1 -hydroxy-ethyl]-piperidine-1 – carboxylic acid tert-butyl ester (100 mg), 1 -methanesulfonyl-piperazine hydrochloride (70 mg), potassium carbonate (100 mg), and N,N-dimethylformamide (1 mL) is stirred for 4 h at 60C. After cooling to room temperature ethyl acetate is added. The organic phase is separated, washed with water and brine, dried over MgS04, and concentrated in vacuo. The residue is chromatographed on silica gel(cyclohexane/ethyl acetate 50:50? 0: 100) to give the title compound. LC (method 7): tR = 1 .46 min; Mass spectrum (EST): m/z = 504 [M+H]+.

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HIMMELSBACH, Frank; ECKHARDT, Matthias; HEINE, Niklas; LANGKOPF, Elke; NOSSE, Bernd; WO2012/80476; (2012); A1;,
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Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 6-bromo-4,7-dichloro-2-methylquinazoline (435 mg, 1.49 mmol) and 1 -tert-butyl 2-methyl piperazine- 1 ,2-dicarboxylate (437 mg, 1.79 mmol) in 1,4-dioxane (30 mL), DIEA (769 mg, 5.96 mmol) was added. The mixture was stirred at 80C for 1.5 h. The mixture was allowed to cool to RT and partitioned between water and ethyl acetate. The organic layer was washed with brine, dried over Na2SO4 and concentrated. The residue was purified by flash column chromatography on silica gel (5-50 % ethyl acetate/petroleum ether) to afford the desired product (224 mg,30 % yield) as a yellow solid.

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARAXES PHARMA LLC; JANES, Matthew, Robert; PATRICELLI, Matthew, Peter; LI, Liansheng; REN, Pingda; LIU, Yi; (397 pag.)WO2016/44772; (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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

A mixture of 1-tert-butyl 3-methyl piperazine-1,3-dicarboxylate (5.133 g, 21.01 mmol), methyl 2,6-dichloropyrimidine-4-carboxylate (4.354 g, 21.03 mmol), and iPr2NEt (4.0 mL, 23.0 mmol) in acetonitrile (50 mL) was heated at 50C for 4 h. After cooling, the reaction mixture was evaporated in vacuo and the residue chromatographed over silica gel with 20-70% EtOAc in hexanes. The product fractions were evaporated in vacuo to give 1-tert-butyl 3-methyl 4-(2-chloro-6-(methoxycarbonyl)pyrimidin-4-yl)piperazine-1,3-dicarboxylate as a very pale yellow powder (6.626 g, 15.97 mmol, 76% yield). LC/MS: m/z= 415.2 [M+H]+.

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; PURDUE PHARMA L.P.; LOCKMAN, Jeffrey; NI, Chiyou; PARK, Jae Hyun; PARK, Minnie; SHAO, Bin; TAFESSE, Laykea; YAO, Jiangchao; YOUNGMAN, Mark, A.; WO2014/135955; (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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

4-Amino-N-[4-[(4-methylpiperazin-1-yl) methyl] phenyl]-1Hpyrazole-3-carboxamide (5): The mixture of N-methylpiperazine (4.9 mL, 44.2 mmol) and triethylamine (12 mL,86.3 mmol) in dichloromethane (20 mL) was added dropwiseto a stirred solution of Nitro-benzyl bromide 1 (10.0 mg,46.3 mmol) in dichloromethane (100 mL) under the ice-waterbath and was refluxed for 1 h. The reaction mixture was extractedwith chloroform (100 mL¡Á3), washed with water andsaturated sodium chloride each time (100 mL¡Á1). The organicphase was dried with anhydrous magnesium sulfate, filtered,evaporated under vacuum to give pale yellow solid 2. Withoutfurther purification, 2 mixed with FeO(OH)/C (catalyst 2.0 g)and 95% ethanol (100 mL) were kept refluxing and dropwiseadded the mixture of hydrazine hydrate (25 mL) and 95%ethanol (20 mL), then filtrated when the solution was hot. Theresidue was washed with hot ethanol (30 mL¡Á2). The solventwas distilled under vacuum to give white solid 3 (6.7 g), thenmixed with 4-nitro-1H-pyrazole-3-acid (6.3 g, 40.0 mmol),EDCI (8.4 g, 43.8 mmol) and HOBT (6.0 g, 44.4 mmol) in anhydrousDMF (100 mL), stirred for 24 h at room temperature.The reaction mixture was poured into ice water (200 mL).A large amount of yellow solid precipitation was acquired.The pure product 4 was got from recrystallizing with mixedsolvent of methanol and ethyl acetate, then the same processof hydrazine hydrate reduction was done with the catalyst ofFeO(OH)/C. The solvent was distilled under vacuum to give white solid 5 (3.5 g). Yield= 63.9%; mp 199-201C; IR (KBr)cm-1: 3369, 3227 (NH2), 1346 (C= C), 1456 (C= N) pyrazole,646 (ArH); 1H-NMR (300 MHz, DMSO-d6) delta (ppm): 2.1 (3H,s, -CH3), 2.3-2.5 (8H, m, -CH2-), 3.3 (2H, s, -CH2-), 4.7(1H, s, -NH2), 7.1-7.2 (3H, m, ArH), 7.7 (2H, d, J=10.5 Hz,ArH), 9.7 (1H, s, -NHCO-), 12.7 (1H, s, Pyrazole); MS m/z:315.82 (M+); Anal. Calcd for C16H22N6O: C, 61.13; H, 7.05; N,26.73; O, 5.09. Found: C, 61.31; H, 6.84; N, 26.52.

The synthetic route of 70261-81-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Lu, Yi; Ran, Ting; Lin, Guowu; Jin, Qiaomei; Jin, Jianling; Li, Hongmei; Guo, Hao; Lu, Tao; Wang, Yue; Chemical and Pharmaceutical Bulletin; vol. 62; 3; (2014); p. 238 – 246;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1: To the product of Preparation 13, Step 3 (0.64 g, 2.2 mmol) in CH2Cl2 (10 ml) add DIPEA (0.57 ml, 3.3 mmol), followed by EtOCOCl (0.26 ml, 2.6 mmol). Stir 0.5 h, concentrate, and purify by PLC to obtain the di-carbamate as a brown oil.

The synthetic route of 154590-35-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Schering Corporation; US2004/220194; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics