Tag: M.W:200-300

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.

129799-08-2, To 1-(1,1-dimethylethyl) 3-methyl piperazine-1,3-dicarboxylate (1.00g, 4.09 mmol) in dry toluene (15 mL) was added 3-bromo-chlorobenzene (653 mg, 3.41 mmol), Pd2(dba)3 (93.0 mg, 0.102 mmol), BINAP (191 mg, 0.307 mmol), and cesium carbonate (1.11 g, 4.77 mmol). The reaction mixture was stirred at 100 C for 42 h, then cooled to room temperature and filtered through celite. The filter cake was washed with ethanol, and the filtrate was concentrated. Column chromatography on silica (hexanes:ethyl acetate 3: 1) provided 1-(1,1-dimethylethyl) 3-methyl 4-(3-chlorophenyl)piperazine-1,3- dicarboxylate (310 mg, 21% yield) as a colorless oil. ?H NMR (400 MHz, CDC13) 8 7.20- 7.13 (t, 1H), 6.84-6.79 (m, 2H), 6.73-6.78 (d, 1H), 4.63-4.50 (br s, 1H), 4.41-4.32 (br s, 1H), 4.24-4.02 (br s, 2H), 3.71-3.65 (s, 3H), 3.55-3.46 (br s, 1H), 3.42-3.26 (br s, 1H), 3.16-2.97 (br s, 1H), 1.49-1.42 (s, 9H); MS (ESI) for C17H23ClN204: 355 (MH(at)).

The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EXELIXIS, INC.; WO2005/117909; (2005); A2;,
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

6-(Thiophen-2-yl) hexanoic acid (77 mg, 0.39 mmol), HOBt (58 mg, 0.43 mmol), TBTU (138 mg, 0.43 mmol), anhydrous triethylamine (87 ??, 0.63 mmol) and dry DMF (2 ml) were placed in an oven-dried Schlenk tube under a nitrogen atmosphere. The resulting solution was stirred at room temperature for 15 minutes. A second Schlenk tube was prepared containing 1-(4-trifluoromethyl phenyl) piperazine (100 mg, 0.43 mmol and dry DMF (1 ml) under a nitrogen atmosphere. The resulting solution was stirred until complete dissolution of the piperazine had occurred. The piperazine solution was then transferred, via a cannula, to the first Schlenk tube containing the carboxylic acid. The resulting solution was stirred for 24 hrs, under nitrogen, and monitored by TLC. After 24 hrs, the DMF was removed under reduced pressure and the resulting oil was acidified using a 0.1 M hydrochloric acid solution. The aqueous mixture was extracted with dichloromethane (20 ml, followed by 4 x 10 ml) and the organic layer washed with a saturated sodium bicarbonate solution (3 x 20 ml) and brine (3 x 20 ml). The organic layer was dried over magnesium sulphate and evaporated under reduced pressure. The residue was purified using flash chromatography (3:2, EtOAc:n-hexane) to obtain the desired product in an 75 % yield. H NMR (300 MHz, CDCI3) ? 7.48 (d, 2H), 7.08 (dd, 1 H), 6.88-6.93 (m, 3H), 6.76-6.77 (m, 1 H), 3.75 (t, 2H), 3.59 (t, 2H), 3.22-3.28 (m, 4H), 2.81 (t, 2H), 2.34 (t, 2H), 1.65-1.77 (m, 4H), 1.44-1.48 (m, 4H). MS (+ESI) calcd for C18 H21 F3 N4 O m/z: [M + Na]+ , 410.1621 ; found 433.1532 [Diff(ppm) = -1.15]., 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NATIONAL UNIVERSITY OF IRELAND, MAYNOOTH; STEPHENS, John; FINDLAY, John; KINSELLA, Gemma; MARTIN, Darren; DEVINE, Robert; VELASCO-TORRIJOS, Trinidad; WO2013/60860; (2013); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

7-Bromo-5-methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridine-2-carbaldehyde (69-1) (1 g, 3.90 mmol) and (R)-tert-butyl 3-methylpiperazine-1-carboxylate (70-1) (0.935 g, 4.67 mmol) were dissolved in DCE (26 mL) and acetic acid (0.266 mL, 4.67 mmol) was added. The reaction was stirred for 30 min and sodium triacetoxyborohydride (4.13 g, 19.5 mmol) was added portionwise. After stirring for 16 hours the reaction was quenched by the slow addition of sat. sodium bicarbonate (100 mL) and extracted with DCM (2 x 100 mL). The combined organics were washed with brine, dried over sodium sulfate and concentrated. The residue was purified by column chromotagraphy (silica, 0-10 % MeOH in DCM) to give (R)-tert-butyl 4-((7-bromo-5- methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridin-2-yl)methyl)-3-methylpiperazine-1-carboxylate (70.2) (1.3 g, 76 %) as a white solid. LC/MS (ES+): m/z 440.8 [M + H]+, 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; C4 THERAPEUTICS, INC.; PHILLIPS, Andrew, J.; NASVESCHUK, Chris, G.; HENDERSON, James, A.; LIANG, Yanke; FITZGERALD, Mark, E.; MICHAEL, Ryan, E.; (790 pag.)WO2017/197056; (2017); A1;,
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Piperazines – an overview | ScienceDirect Topics

694499-26-8,694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

to a solution of HSD1251 (50 mg, 0.18 mmol) in DMF (2.5 mL) was added 4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (0.19 mmol), HATU (0.18 mmol), and DIPEA (0.39 mmol). Reaction was continued for 12 h at room temperature and monitored by TLC. After completion, reaction mixture was extracted with ethyl acetate and washed with brine solution and dried over Na2S04. Crude was purified with flash chromatography to get the desired product as Off-white solid (50% yield, 47 mg1H NMR (500 MHz, DMSO-6) delta 10.93 (s, 1H), 8.63 (s, 1H), 8.29 (d, = 2.2 Hz, 1H), 8.05 (dd, = 8.5, 2.3 Hz, 1H), 7.98 – 7.89 (m, 2H), 7.71 (d, = 8.5 Hz, 1H), 3.56 (s, 2H), 3.34 – 3.30 (m, 2H), 3.13 (t, = 6.2 Hz, 2H), 2.37 (s, 8H), 2.14 (s, 3H), 1.99 (ddt, = 8.9, 6.3, 2.9 Hz, 2H), 1.87 – 1.79 (m, 2H);13C NMR (126 MHz, DMSO) delta 166.54, 149.19, 143.71, 142.60, 138.52, 132.53, 131.81, 129.74, 129.42, 128.11 (q, = 28.9 Hz), 125.91(q, = 274.6 Hz), 123.78, 123.53, 117.19, 117.14, 116.03, 57.94, 55.22, 53.19, 46.22, 29.73, 26.89, 22.37, 22.07; HRMS (ESI) m/z calcd for C28H30F3N6O [M + H]+523.2433, found 523.2433.

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference£º
Patent; PURDUE RESEARCH FOUNDATION; SINTIM, Herman O.; DAYAL, Neetu; OPOKU-TEMENG, Clement; (195 pag.)WO2018/183586; (2018); A1;,
Piperazine – Wikipedia
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,129799-15-1

A mixture of (S) -5- (1- ( (tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4- (difluoromethoxy) phenyl) oxazole-4-carboxylic acid (0.25 g, 0.53 mmol) , 1-tert-butyl 2-methyl piperazine-1, 2-dicarboxylate (157 mg, 0.64 mmol) , EDCI (153 mg, 0.80 mmol) and HOAT (181 mg, 1.33 mmol) in DCM (20 mL) was stirred at 0 , and DIPEA (0.37 mL, 2.13 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 5 h. The mixture was concentrated. The residue was purified by silica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 3/1 to give the title compound as colorless thick oil (260 mg, 70) .1H NMR (400 MHz, CDCl3) : delta ppm 7.55-7.62 (m, 2H) , 7.26 (d, J 8.4 Hz, 1H) , 6.72 (t, JF-H 75.1 Hz, 1H) , 5.25-5.29 (m, 1H) , 3.97-4.01 (m, 3H) , 3.79 (br. s, 1H) , 3.58-3.63 (m, 2H) , 1.50-1.52 (m, 3H) , 1.48 (s, 9H) , 1.45 (s, 9H) , 1.32-1.35 (m, 1H) , 0.68-0.73 (m, 2H) , 0.42-0.44 (m, 2H) and MS-ESI: m/z 695.3 [M+H] +.

As the paragraph descriping shows that 129799-15-1 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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 7-benzyl-2,4-dichloro-6,8- dihydro-5H-pyrido[3,4-d] pyrimidine (2.00 g, 6.80 mmol, 1.00 eq) in DMSO (40.0 mL) was added DIEA (1.76 g, 13.6 mmol, 2.38 mL, 2.00 eq) and 1-tert-butyl 2-methylpiperazine-l,2- dicarboxylate (1.74 g, 7.14 mmol, 1.05 eq). The mixture was stirred at 55 C for 16 hours. The mixture was diluted with water (100 mL) and extracted with ethyl acetate (3 x 100 mL). The combined organic layers were washed with brine (3 chi 100 mL), dried over Na2S04, filtered and concentrated to dryness. The residue was purified by column chromatography (S1O2, diethyl ether/ethyl acetate = 1 :0 to 3 : 1) to give 1-tert-butyl 2-methyl-4-(7-benzyl-2-chloro-6,8-dihydro- 5H-pyrido[3,4-d]pyrimidin -4-yl)piperazine-l,2-dicarboxylate (3.10 g, 5.70 mmol, 83.8 % yield, 92.3 % purity) as a yellow semisolid. ESI MS m/z 502.2 [M+H]+.

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

Reference£º
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; FISCHER, John, P.; FELL, Jay, Bradford; BLAKE, James, F.; HINKLIN, Ronald, Jay; MEJIA, Macedonio, J.; HICKEN, Erik, James; CHICARELLI, Mark, Joseph; GAUDINO, John, J.; VIGERS, Guy, P.A.; BURGESS, Laurence, E.; MARX, Matthew, Arnold; CHRISTENSEN, James, Gail; LEE, Matthew, Randolf; SAVECHENKOV, Pavel; ZECCA, Henry, J.; (529 pag.)WO2017/201161; (2017); 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

The compound 11 (248.0 mg, 1 . 0mmol) and sodium iodide (180.0 mg, 1 . 2mmol) is added to methanol (10.0 ml) and stirring, and then adding substituted amine (2.1mmol) and heating to 40 C reaction 3 – 6 hours, TLC monitoring display complete raw material reaction, concentrated, column chromatography to obtain compound 12, wherein R4 With the corresponding product in the definition of the same.

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; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Yang Chunhao; Miao Zehong; Yue Zhizhou; Liang Yukun; Feng Jianming; Li Jiaxin; He Qian; (30 pag.)CN104250246; (2017); B;,
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.

General procedure: To a solution of carboxylic acid (50 mmol) in DMF (0.25 mL) in a 48 position Mettler Toledo XT reaction block was added PyBOP (50 mmol, 0.2 mL of 0.3 M solution in DMF) and TEA (75 mmol, 0.05 mL of 1.5 M solution in DMF) followed by the appropriate amine build blocks (55 mmol, 0.55 ml of 1 M solution in DMF). The reactions were stirred at rt 24 h and concentrated by GeneVac HT-4 to remove all reaction mixture including excess amine and DMF. The crude mixtures were dissolved in EtOAc (1 mL) and filtered through silica-packed short-column and washed with EtOAc (3 mL). The collected organic solution was concentrated in GeneVac HT-4 and dissolved in DMSO (1 mL). DMSO solution was subjected to HTAC for pre-purification analysis, purification, and final QC., 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; Hwang, Jong Yeon; Attia, Ramy R.; Carrillo, Angela K.; Connelly, Michele C.; Guy, R. Kiplin; Bioorganic and Medicinal Chemistry Letters; vol. 23; 6; (2013); p. 1891 – 1895;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-81-3,70261-81-3, 1-Methyl-4-(4-nitrobenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 4-Nitrobenzyl bromide (46.3mmol) was dissolved in dichloromethane (100mL). The solution was added to the mixture of relative amine (47.0mmol) and triethylamine (70.3mmol) in dichloromethane (20ml). The reaction mixture was stirred at r. t. for 24 h and was extracted with dichloromethane (100ml¡Á3). After removal of the solvent, the residue was crystallized from ethanol, giving yellow powder. Compounds 1 and 2 were used for further reaction without purification. To a suspension of compounds 1-2 (36.2mmol) in 95% ethanol (100ml), 85% NH2NH2¡¤H2O (362mmol), 95% ethanol (100ml) and iron (III) oxide hydroxide (FeO(OH)/C, 2.0g) were added and heated to reflux. When TLC analysis showed complete conversion of the starting material, the reaction mixture was filtrate through Cellit and the filtrate was concentrated in vacuum. The crude product was purified by silica gel colum chromatography (DCM/MeOH) to yield the title compound (3 and 4) as white solid. The mixture of compound 4 (1eq, 18.5mmol), 4-Nitro-1H-pyrazole-3-acid (1.1equiv, 20.4mmol), EDC (1.2equiv, 22.2mmol), HOBT (1.2equiv, 22.2mmol) in DMF (50ml) was stirred for 24h. The ice water (100ml) was added to the reaction mixture. A large amount of yellow solid precipitation (compound 8) was acquired. Compound 8 was used without further purification. Compounds 8 was reduced by the same process as compound 4, and then the resulting compound 12 was purified by column chromatography on silica gel, eluted with the appropriate solvent.

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Article; Zhi, Yanle; Li, Baoquan; Yao, Chao; Li, Hongmei; Chen, Puzhou; Bao, Jiyin; Qin, Tianren; Wang, Yue; Lu, Tao; Lu, Shuai; European Journal of Medicinal Chemistry; vol. 155; (2018); p. 303 – 315;,
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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.123987-13-3,(3-(4-Methylpiperazin-1-yl)phenyl)methanol,as a common compound, the synthetic route is as follows.

A mixture of thionyl chloride (87 mg, 0.727 mmol) and (3-(4-methylpiperazin-l- yl)phenyl)methanol (30.0 mg, 0.145 mmol) in DCM (10 mL) was heated to 60 C for 2 h. The mixture was then concentrated under reduced pressure to a foam, which was used for the next step without further purification. MS(ES+) Ci2HisN20 requires: 224, found: 225 [M+H]+., 123987-13-3

As the paragraph descriping shows that 123987-13-3 is playing an increasingly important role.

Reference£º
Patent; JONES, Philip; DIFRANCESCO, Maria, Emilia; PETROCCHI, Alessia; MARSZALEK, Joe; LIU, Gang; KANG, Zhijun; CARROLL, Christopher, L.; MCAFOOS, Timothy; CZAKO, Barbara; WO2014/31928; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics