Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.67455-41-8,4-(Piperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

To a dark transparent solution of 1-(4-aminophenyl)piperazine (300 mg, 1.693 mmol) and triethylamine (0.236 mL, 1.693 mmol) in DCM (30 mL) was added benzyl chloroformate (0.238 mL, 1.693 mmol) dropwise with stirring. The resulting solution was allowed to stir at rt for 1 h, after which HPLC showed reaction completion. Concentration and CombiFlash (10 g, DCM to 10% MeOH/DCM) afforded Cmpd AG as a solid. 1H-NMR (300 MHz, CDCl3) 7.35 (m, 5H), 4.80 (d, J=8.8 Hz, 2H), 6.66 (d, J=8.8 Hz, 2H), 5.16 (d, 2H), 3.65 (m, 4H), 3.49 (br-s, 2H), 2.99 (br-s, 4H), 67455-41-8

The synthetic route of 67455-41-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Vankayalapati, Hariprasad; Liu, Xiao-Hui; Hewitt, William Merton; Gourley, Eric Scott; Xu, Yong; Aavula, Bhasker; US2010/204221; (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.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

Intermediate 33: Step a 1-(6-(4-Cyclopropylpiperazin-1-yl)pyridin-3-yl)ethanone A solution of 1-cyclopropylpiperazine (0.162 g, 1.29 mmol), 1-(6-chloropyridin-3-yl)ethanone (0.200 g, 1.29 mmol) and DMSO (0.2 mL) was heated to 100 C. overnight. The reaction was cooled to room temperature, ethyl acetate was added and the reaction mixture was filtered to give the title compound as a solid., 20327-23-5

As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

Reference：
Patent; ZHANG, Yan; Tounge, Brett Andrew; Wang, Aihua; Hawkins, Michael; Leonard, Kristi Anne; Barbay, Joseph Kent; Maharoof, Umar S.M.; US2012/129843; (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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Under an argon atmosphere, 3,4-difluoronitrobenzene(1.0 g, 6.29 mmol) in acetonitrile (15 mL)To the solution was added cis-3,5-dimethylpiperazine (861 mg, 7.55 mmol), N, N-diisopropylethylamine (2.19 mL,12.6 mmol), and the mixture was stirred at 80 ° C. for 2 hours.Water was added to the reaction solution, and the mixture was extracted with chloroform.The chloroform layer was washed with saturated brine and saturated brine,After drying over anhydrous magnesium sulfate, filtration,The solvent was distilled off. The resulting residue was purified by silica gel column chromatography (NH column, chloroform / methanol) to give the title compound (1.42 g, 89percent)., 21655-48-1

The synthetic route of 21655-48-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Yakult Honsha Corporation; Abe, Atsuhiro; Mae, Satoyuki; Yamazaki, Ryuta; Sawaguchi, Yuichi; Sugimoto, Takuya; Sasai, Toshio; Nishiyama, Hiroyuki; Nagaoka, Masato; Matsuzaki, Ken; Kurita, Akinobu; Matsui, Makoto; Shingeyama, Takahide; (208 pag.)JP6378918; (2018); B2;,
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.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

Reference Example 46] 1-Methylpiperazin-2-one [Show Image] An aqueous 1 N sodium hydroxide solution was added to a suspension of 1-methylpiperazin-2-one hydrochloride (19.6 g) of Reference Example 21-(3) in dichloromethane, and the resultant mixture was partitioned. Further, sodium chloride was added to the aqueous layer to saturate the layer, and then the aqueous layer was extracted with dichloromethane. The organic layers were combined and dried over anhydrous sodium sulfate. After separation by filtration, the solvent was evaporated under reduced pressure, and the title compound (5.90 g) was obtained as an oily product. ESI-MSm/z: 115(M+H)+.

109384-27-2, 109384-27-2 1-Methylpiperazin-2-one hydrochloride 17060766, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1785418; (2007); 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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: In an oven-dried RB flask, 4-chloro-2-phenyl-1H-pyrrolo[3,2-c]pyridine 6b (250 mg, 1.09 mmol) and formaldehyde solution, 37 wt.percent in H2O (0.2 mL, 2.73 mmol) were mixed in glacial acetic acid(5 mL). N-methyl piperazine (273.8 mg, 2.73 mmol, CAS 109-01-3)was added drop wise at 0°C. The resulting mixture was stirred atroom temperature for 12 h. After completion of the reaction, the excess solvent was evaporated to dryness under reduced pressure.The residue was neutralized with 10percent NaHCO3 solution, the solidf ormed was collected by filtration, washed with water and dried.The crude product was purified by silica gel column chromatographyto provide title compound as an off-white solid (326.3 mg,88percent)., 4318-42-7

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Jose, Gilish; Suresha Kumara, Tholappanavara H.; Sowmya, Haliwana B.V.; Sriram, Dharmarajan; Guru Row, Tayur N.; Hosamani, Amar A.; More, Sunil S.; Janardhan, Bhavya; Harish; Telkar, Sandeep; Ravikumar, Yalegara Siddappa; European Journal of Medicinal Chemistry; vol. 131; (2017); p. 275 – 288;,
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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Preparation 6 (5-Bromo-l,2-benzothiazol-7- l)-[cz5,-3,5-dimethylpiperazin-l-yl]methanone To a mixture of 5-bromo-l,2-benzothiazole-7-carboxylic acid (10 g, 0.039 mol) and DMF (100 mL) is added cw-2,6-dimethylpiperazine (6.64 g, 0.058 mol) at 28 °C. The resulting mixture is cooled to 0 °C and HATU (22.1 g, 0.058 mol) is added in portions (internal temperature is 0 to 2 °C). The mixture is warmed to 25 °C and stirred at this temperature for 16 h. The mixture is concentrated under vacuum, poured into water (30 mL) and extracted with ethyl acetate (3 chi 50 mL). The combined organic portions are washed with saturated sodium bicarbonate solution (30 mL) and brine (30 mL). The organic portion is concentrated and the resulting residue is dissolved in a mixture of dichloromethane (30 mL) and water (30 mL). 6 N HC1 is added dropwise until a majority of the solid appears. The solid is collected by filtration. The aqueous phase of the filtrate is separated and combined with the solid cake, basified with sodium bicarbonate solution to pH 8, and then extracted with dichloromethane (3 chi 50 mL). The organic phase is concentrated to give the title compound (10.1 g, 74percent). LC-ES/MS m/z (79Br/81Br) 354/356 [M+H]+., 21655-48-1

As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference：
Patent; ELI LILLY AND COMPANY; GENIN, Michael James; HOLLOWAY, William Glen; REKHTER, Mark David; (41 pag.)WO2016/81311; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74879-18-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: To a stirred mixture of homopiperazine (0.60 g, 6.00 mmol), 4-fluorobenzaldehyde (0.60 g, 5.00 mmol) in DCM (15 mL) wasadded AcOH (0.08 mL, 0.50 mmol) and the mixture was stirred atroom temperature for 0.5 h. Then sodium triacetoxyborohydride(1.60 g, 7.50 mmol) was added in portions. The reaction was stirredat the same temperature for 6 h. Finally, the mixture was dilutedwith saturated aqueous NaHCO3 (15.00 mL) followed by water(15.00 mL) and extracted with EtOAc (3 15.00 mL). The organiclayer was dried (MgSO4), filtered, and concentrated in vacuo. Theresidue was purified by column chromatography on silica gel (EtOAc/PE 5:1) to afford yellow oil (0.90 g, yield 77%).

74879-18-8 (S)-(+)-2-Methylpiperazine 2734219, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Hu, Suwen; Wang, Zhilong; Hou, Tingjun; Ma, Xiaodong; Li, Jing; Liu, Tao; Xie, Xin; Hu, Yongzhou; Bioorganic and Medicinal Chemistry; vol. 23; 5; (2015); p. 1157 – 1168;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Comparative example 6 A reaction was carried out as described for Example 6, except that the solvent was changed from 44 g of ethanol to a mixed solvent consisting of 22 g of water and 22 g of ethanol (water content 50.0 wt%). As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 37.7% (based on the amount of 2-methylpiperazine)., 109-07-9

The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (2005); 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.1152367-80-0,(S)-1,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Part A 2-[(2S)-2,4-Dimethyl-1-piperazinyl]-4-pyrimidinamine A mixture of 2-chloro-4-pyrimidinamine (200 mg, 1.544 mmol), Hunig’s base (1348 mul, 7.72 mmol) and (3S)-1,3-dimethylpiperazine (Ref.: WO2009061879 (A1)) (318 mg, 1.698 mmol) in N,N-dimethylformamide (DMF) (1.7 ml) was heated to 220 C. via a microwave reactor for 15 min. The reaction mixture was purified by RP-HPLC to yield 2-[(2S)-2,4-dimethyl-1-piperazinyl]-4-pyrimidinamine (88 mg, 0.425 mmol, 28% yield). MS (ES+) m/z 208.0 (MH+).

1152367-80-0, 1152367-80-0 (S)-1,3-Dimethylpiperazine 13152036, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GlaxoSmithKline Intellectual Property (No. 2) Limited; Aubart, Kelly M.; Benowitz, Andrew B.; Fang, Yuhong; Hoffman, James; Karpinski, Joseph M.; Knox, Andrew Nicholson; Liao, Xiangmin; Qin, Donghui; Shi, Dongchuan; Spletstoser, Jared T.; US8901119; (2014); B2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To mixture of (2S)(‘/WJ-5-(-1-(tert-butoxy)-2-methoxy-2-oxoethyl)-4-(8-fluoro-5-methylchroman- 6-yl)-1 ,6-dimethyl-1 H-pyrrolo[2,3-b]pyridine-2-carboxylic acid (30 mg, 0.060 mmol) and 1- cyclopentylpiperazine (8.67 pL, 0.060 mmol) in ethyl acetate (1 mL) was added DIEA (0.026 mL, 0.150 mmol) followed by addition of 1-propanephosphonic acid cyclic anhydride (T3P) (0.072 mL, 0.120 mmol) as a 50% solution in ethyl acetate and stirred at room temperature for 30 min. Diluted with ethyl acetate, added water and saturated ammonium chloride and extracted with ethyl acetate. Organic phase was washed with brine, dried over IS^SC^, filtered and concentrated to give (2S (7WJ-methyl 2-(tert-butoxy)-2-(2-(4-cyclopentylpiperazine-1-carbonyl)-4- (8-fluoro-5-methylchroman-6-yl)-1 ,6-dimethyl-1 H-pyrrolo[2,3-b]pyridin-5-yl)acetate (37 mg, 97% yield) as a colorless oil. 1H NMR (400 MHz, CHLOROFORM-d) delta = 6.74 (br. s., 1 H), 5.99 (br. s., 1 H), 5.14 (s, 1 H), 4.32 (t, J=5.0 Hz, 2 H), 3.93 (br. s., 3 H), 3.78 – 3.88 (m, 1 H), 3.59 (s, 3 H), 2.78 – 2.86 (m, 3 H), 2.74 (br. s., 2 H), 2.53 (br. s., 2 H), 2.17 (br. s., 2 H), 1.89 (br. s., 2 H), 1.78 (s, 3 H), 1.57 (br. s., 12 H), 1.06 – 1.17 (m, 9 H); LC/MS (m/z) ES+ = 635 (M+1)

21043-40-3, The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; VIIV HEALTHCARE UK LIMITED; DE LA ROSA, Martha Alicia; JOHNS, Brian, Alvin; KAZMIERSKI, Wieslaw, Mieczyslaw; SAMANO, Vicente; SUWANDI, Lita; TEMELKOFF, David; VELTHUISEN, Emile; WEATHERHEAD, Jason, Gordon; WO2014/9794; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics