Tag: M.W:200-300

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.

Step A: Amination of halopyrazine; Preparation of 2-amino-5-bromo-3-r(S)-4-Boc-3-benzylpiperazinyllpyrazine 108; To a solution of 2-arnino-3,5-dibromopyrazine 106 (0.2 g, 0.79 mmol.) and (S)- 1 -Boc-2-benzylpiperazine 107 (0.44 g, 1.59 mmol) in dioxane (2 ml_) and trifluoromethylbenzene (2 ml_) was added diisopropylethylamine (0.31 g, 2.4 mmol). The reaction mixture was heated in a microwave reactor at 210 0C for 20 minutes. Ethyl acetate (100 ml_) was added. The organic layer was washed with water and brine. The organic layer was dried over sodium sulfate. The organic solvent was evaporated under reduced pressure. The crude product was purified by RP-HPLC to yield the desired 2-amino-5-bromo-3-[(S)-4-Boc-3-benzylpiperazinyl]pyrazine 108 (0.24 g, 0.536 mmol).

169447-86-3, 169447-86-3 (S)-tert-Butyl 2-benzylpiperazine-1-carboxylate 17750441, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SCHERING CORPORATION; WO2007/126964; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

106261-48-7, 4-((4-Methylpiperazin-1-yl)methyl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 12: 4-( 4-Methvl-piperazin-1-vlmethvl)-N-r 4-(5-thiophen-3-vl-pvrimidin-2-vlamino )-phenvll- benzamide; 4-Chloromethylbenzoic acid (1.7 g, 10 mmol) and 2.78 mL (20 mmol) of triethylamine in 50 mL of dimethylformamide was stirred with 1.22 mL (11 mmol) of N-methylpiperazine overnight at room temperature. The white solid was collected by vacuum filtration and washed with dichloromethane. The combined filtrates were rotary evaporated to dryness to give 4-(4-methyl-piperazin-1-ylmethyl)-benzoic acid. N-(5-Thiophen-3-yl-pyrimidin-2-yl)-benzene-1 ,4-diamine (55 mg, 0.20 mmol), triethylamine (0.112 mL, 0.80 mmol), BOP reagent (265 mg, 0.6 mmol) and 93 mg (0.4 mmol) of 4-(4-methyl-piperazin-1- ylmethyl) -benzoic acid in 1 mL of dimethylformamide were stirred overnight at room temperature. The solvent was evaporated and the residue purified by flash chromatography eluting with dichloromethane:methanol 20: 1 and then dichlormehane:methanol 15: 1 to give 4-(4-methyl-piperazin-1- ylmethyl)-N[4-(5-thiophen-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide. H-NMR (dimethylsulfoxide-d6) 8 10.03 (s, 1 H), 9.65 (s, 1 H), 8.80 (s, 2H), 7.85 (m, 3H), 7.67 (m, 2H), 7.63 (m, 2H), 7.57 (d, 1 H), 7.38 (d, 2H), 3.45 (s, 2H), 2.50 (m, 8H), 2.30 (s, 3H). MS (m/z) 485 [M+1]., 106261-48-7

As the paragraph descriping shows that 106261-48-7 is playing an increasingly important role.

Reference：
Patent; SUGEN, INC.; WO2005/113548; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

106261-48-7, 4-((4-Methylpiperazin-1-yl)methyl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The mixture containing compound 6 (2.51 mmol), methanol (5.0 mL), 2 M NaOH (1.6 mL) was stirred at room temperature for 4 h, concentrated under reduced pressure and acidified with concentrated hydrochloric acid to pH 2. The aqueous phase was concentrated to dryness under reduced pressure to afford the crude 4-aminomethylbenzoic acid (containing sodium chloride) which was carried on the next step without further purification. The 4-aminomethylbenzoic acid (2.51 mmol) and 2 drops of DMF were added to thionyl chloride (10 mL). The mixture was refluxed for2 h. The volatile was removed under reduced pressure to give a pale yellow solid which was then dissolved in anhydrous THF (10 mL) and was added dropwise to a suspension of sodium azide (0.24 g, 3.77 mmol) in 10 mL of THF/H2O (4:1, v/v) at 0-5C. Then the mixture was stirred at room temperature overnight and THF was removed under reduced pressure. The aqueous phase was extracted with dichloromethane (20 mL 3). The organic layerwas combined, washed with brine (20 mL), dried (Na2SO4), filtered and concentrated under reduced pressure to produce compounds 7a-7f as yellow or brown oil., 106261-48-7

Big data shows that 106261-48-7 is playing an increasingly important role.

Reference：
Article; Zuo, Sai-Jie; Zhang, Sai; Mao, Shuai; Xie, Xiao-Xiao; Xiao, Xue; Xin, Min-Hnag; Xuan, Wei; He, Yuan-Yuan; Cao, Yong-Xiao; Zhang, San-Qi; Bioorganic and Medicinal Chemistry; vol. 24; 2; (2016); p. 179 – 190;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(c) 4-Methyl-N-(4-((4-methylpiperazin-l-yl)methyl)phenyl)-3-(4-phenylpyrimidin-2- ylamino)benzamide[0071] DIEA (50muL, 0.204mmol) was added into a solution of 3-bromo-4- methylbenzoic acid (15mumg, 0.049mmol), 4-((4-methylpiperazin-l-yl)methyl)benzenamine (9mg, 0.04mmol), BOP (25mg, 0.057mmol) in DMF. The reaction mixture was stirred at rt under argon atmosphere overnight. The reaction mixture was then purified by a semi- preparative HPLC to give pure product as white powder. MS (ESI+) m/z 493.2 [M+H]+.

70261-82-4, As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role.

Reference：
Patent; INTRA-CELLULAR THERAPIES, INC.; WO2008/153959; (2008); 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.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of terf-butyl 4-carbamothioylpiperazine-1-carboxylate (synthesized according to Example 5, Step 1, 3.0 g, 12 mmol) in dioxane (10 mL), TEA (2.6 mL, 16 mmol) and 3-bromo-ethyl pyruvate (2.1 mL, 16 mmol) were added at rt and the mixture was stirred at 90 C for 16 h. The completion of the reaction was monitored by TLC. The reaction mixture was quenched with water and extracted with EtOAc. The organic layer was dried over anhydrous Na2SO4, concentrated under vacuum and the resulting crude product was taken as such for next step. Yield: 95% (4 g, black solid).

196811-66-2, As the paragraph descriping shows that 196811-66-2 is playing an increasingly important role.

Reference：
Patent; ASCENEURON SA; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; (243 pag.)WO2016/30443; (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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of tert-butyl (2S)-2- methylpiperazine-l-carboxylate (400 mg, 2.00 mmol) in dichloromethane (6 mL) was added acetic acid (120 mg, 2.0 mmol) and 5-cyclopropyl-3-(2,6-dichlorophenyl)-l,2-oxazole-4- carbaldehyde (562 mg, 1.99 mmol). After the mixture was stirred for 30 min, NaBH(OAc)3 (1.3 g, 6.13 mmol) was added. The resulting solution was stirred overnight at room temperature. The solids were filtered out. The resulting mixture was concentrated under vacuum. The residue was applied onto a silica gel column with ethyl acetate/petroleum ether (30:70). This resulted in 670 mg (72%) of the title compound as a white solid. LC-MS (ESI, m/z): [M+H]+ = 466.2., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; HEPAGENE THERAPEUTICS, INC.; XU, Xiaodong; (104 pag.)WO2018/85148; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

77279-24-4,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.77279-24-4,tert-Butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Weigh the compound 10 (8.7 g, 37.8 mmol) in anhydrous tetrahydrofuran (THF)Then, dimethylaminopyridine DMAP (0.23 g, 1.9 mmol) and triethylamine (4.9 g, 49 l lm) were added; methanesulfonyl chloride (5.2 g, 45.3 mml) was added dropwise to the ice bath After the completion of the solution slowly rose to room temperature for 5h; TLC detection, iodine cylinder color; until the raw material disappeared after adding a small amount of ice water quenching, recovery solvent was crude, silica gel column chromatography (petroleum ether / ethyl acetate) 3.9 g)

As the paragraph descriping shows that 77279-24-4 is playing an increasingly important role.

Reference：
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

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

General procedure: To a solution of 3-iodo-4-methylbenzoyl chloride obtained above in dry DCM (10mL) at 0C was added Et3N (0.28mL, 2.0mmol) and 4-((4-methylpiperazin-1-yl) methyl)-3-(trifluoromethyl) aniline (328mg, 1.2mmol). The mixture was stirred at room temperature for 5h, and then the solvent was removed under reduced pressure. The residue was purified by using column chromatography to afford the corresponding product 6-1 (439mg, 2 steps yield: 85%)., 694499-26-8

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Liu, Yang; Peng, Xia; Guan, Xiaocong; Lu, Dong; Xi, Yong; Jin, Shiyu; Chen, Hui; Zeng, Limin; Ai, Jing; Geng, Meiyu; Hu, Youhong; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 122 – 132;,
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.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

70261-82-4, A. 8-Indan-5-yl-2-[4-(4-methyl-piperazin-1-ylmethyl)-phenylamino]-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester 8-indan-5-yl-2-methanesulfonyl-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester (0.098 g, 0.24 mmol) and 4-(4-methyl-piperazin-1-ylmethyl)-phenylamine (0.049 g, 0.24 mmol) were combined in i-PrOH (2 mL) and heated to 90 C. After 3 h, the reaction mixture was concentrated and purified by preparative HPLC (30 mL/min 5-100% MeCN/H2O gradient over 10 min) and lyophilized to provide 20 mg of 8-Indan-5-yl-2-[4-(4-methyl-piperazin-1-ylmethyl)-phenylamino]-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester. 1H NMR (400 MHz, CDCl3) delta (ppm): 9.36 (s, 1H), 8.54 (s, 1H), 7.43 (d, 2H, J=7.9 Hz), 7.29 (m, 2H), 7.18 (dd, 2H, J=2.0 Hz, J=7.9 Hz), 7.03-7.05 (m, 1H), 4.38 (q, 2H, J=7.1 Hz), 3.44 (s, 2H), 3.08 (t, 2H, J=7.4 Hz), 3.01 (t, 2H, J=7.5 Hz), 2.52 (br s, 8H), 2.36 (s, 3H), 2.19-2.29 (m, 2H), 1.39 (t, 3H, J=7.1 Hz).

The synthetic route of 70261-82-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Player, Mark R.; Huang, Hui; Hutta, Daniel A.; US2007/60577; (2007); 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

In 5 mL of acetonitrile was dissolved 500 mg (1.693 mmol) of 11-piperazin-l- yldibenzo[b,fj[l,4]thiazepine. Ih 5 mL of acetonitrile was dissolved 254 mg (1.693 mmol) of L- tartaric acid with heating. The solutions were combined and a slightly gummy solid precipitated immediately. The mixture was diluted with an additional 5 mL of acetonitrile. The solid did not dissolve, but triturated into a free-flowing solid. The mixture did not change overnight. The solids were collected, washed with acetonitrile (5 mL), and dried under vacuum at 40 0C resulting in 707 mg crystalline solid (93.8%). mp 170-175 0C (dec). 1H NMR (DMSOd6) was consistent with the title salt.Polarized light microscopy showed that the solid was composed of irregularly shaped crystalline particles. DSC revealed two broad endotherms at 118.3 and 175.1 0C (Figure 1). The lower temperature endothermic event is likely due to water loss and the higher temperature endothermic event may be due to a melt followed by decomposition. TGA revealed two weight loss transitions (Figure 1). The lower temperature weight loss transition coincided with the lower temperature DSC event and was measured to correspond to approximately 1 mole equivalent of water. The higher weight loss transition coincided with the higher DSC event. Dynamic vapor sorption (DVS) studies indicated that the salt was hygroscopic (Figure 2). Moisture gain was reversible with little hysteresis and amounts to about 1 mole equivalent at 90% RH which was in addition to the moisture already contained in the salt., 5747-48-8

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

Reference：
Patent; ASTRAZENECA AB; WO2007/62336; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics