Month: June 2021

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

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

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.150407-69-5,(S)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

Step A – Preparation of Int Int 48-1 To a solution of piperazine carboxylic acid (10 g, 27 mmol) in DCM (50 mL) was added TEA (2.39 mL, 54 mmol) and HATU (11.4 g, 30 mmol) with stirring. The reaction mixture was stirred at room temperature for 30 mins then treated with piperidine (2.57 g, 30 mmol). The reaction solution was stirred for 48 hrs then concentrated. The residue was purified by column chromatography on silica gel eluted with petroleum ether / EtOAc (3 : 1) to afford compound Int 48-1 as yellow oil (10.7g). MS-ESI (m/z): 432 (M+l)+ R 0.6 (PE : EtOAc= 1 : 1) H NMR (CDC13) delta: 7.30-7.24 (m, 5H), 5.25 (s, 1H), 5.14 (d, J=12.3 Hz, 1H), 5.06-4.98 (m, 1H), 4.18-3.80 (m, 5H), 3.41 (s, 2H), 3.21 (d, J=13 Hz, 3H), 1.61 (s, 2H), 1.52 (t, J7=16.6 Hz,, 150407-69-5

As the paragraph descriping shows that 150407-69-5 is playing an increasingly important role.

Reference：
Patent; MERCK SHARP & DOHME CORP.; COBURN, Craig, A.; MALETIC, Milana, M.; LUO, Yunfu; QI, Zhiqi; YU, Tingting; SOLL, Richard; WO2015/73310; (2015); 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

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

217 mg (1 mmol) of alkaloid and 183 mg (1.5 mmol)Monopiperazine hydrochloride was added to 10 mL of methanol and 62 mg (0.1 mmol)In the mixed system of Yb(OTf)3, the reaction was stirred at room temperature for 3 days, and the reaction was completed by TLC.Add 100 mg (1.2 mmol) of NaHCO3 powder and continue to stir for 12 h.Concentrate to dryness under reduced pressure and add 10 mL of benzene to residue.After stirring for 10 min, it was quickly demineralized by a neutral Al2O3 column, concentrated, and purified by silica gel column chromatography (benzene: acetone: ammonia = 10:1:2) to obtain intermediate (III) in a yield of 79%.

142-64-3, As the paragraph descriping shows that 142-64-3 is playing an increasingly important role.

Reference：
Patent; Shijiazhuang College; Zhang Baohua; Shi Lanxiang; (8 pag.)CN109776575; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7,4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: In an oven-dried RB flask, compound 6c (250mg, 1.01mmol) and formaldehyde solution, 37?41wt.percent in water (0.15mL, 2.02mmol) were mixed in glacial acetic acid (5mL). Morpholine (220.4mg, 2.53mmol) was added drop wise at 0°C. The resulting mixture was stirred at room temperature for 12h. After completion of the reaction, the excess solvent was evaporated to dryness under reduced pressure. The residue was neutralized with 10percent NaHCO3 solution, the solid formed was collected by filtration, washed with water and dried. The crude product was purified by silica gel column chromatography to provide title compound.

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference：
Article; Jose, Gilish; Kumara, T. H. Suresha; Nagendrappa, Gopalpur; Sowmya; Jasinski, Jerry P.; Millikan, Sean P.; More, Sunil S.; Janardhan, Bhavya; Harish; Chandrika; Journal of Molecular Structure; vol. 1081; (2015); p. 85 – 95;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5317-33-9, 3-(4-Methylpiperazin-1-yl)propan-1-ol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5317-33-9

b. 7-[3-(4-Methyl-piperazin-1-yl)-propoxy]-4-piperidin-4-yl-quinazoline; Solid KOtBu (1.36 g, 12.1 mmol) was added in one portion under air to a homogeneous solution of 4-(7-Fluoro-quinazolin-4-yl)-piperidine-1-carboxylic acid tert-butyl ester (3.33 g, 10.1 mmol), as prepared in the preceding step, and commercial 3-(4-methyl-piperazin-1-yl)-propan-1-ol (1.50 g, 9.50 mmol) in dry THF (10 mL), while stirring on an ice bath. Following KOtBu addition, the ice bath was immediately removed, and the resulting homogeneous amber solution was stirred for 6 hr. 6 M aqueous HCl (10 mL, 60 mmol) was then added in one portion, and the reaction was stirred overnight (mild bubbles were seen following HCl addition, but these subsided after 15 min). The reaction was then partitioned with 9:1 DCM/MeOH (50 mL) and 2.5 M NaOH (28 mL, 70 mmol), and the aqueous layer was extracted with 9:1 DCM/MeOH (1×50 mL). The combined organic layers were dried (Na2SO4) and concentrated by rotary evaporation at 90 C. to provide the crude title compound as a clear yellow oil (3.79 g, ?102%? crude yield). LC/MS (ESI): calcd mass 369.3, found 370.2 (MH)+.

The synthetic route of 5317-33-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Baindur, Nand; Gaul, Michael David; Kreutter, Kevin Douglas; Baumann, Christian Andrew; Kim, Alexander J.; Xu, Guozhang; Tuman, Robert W.; Johnson, Dana L.; US2006/281772; (2006); 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.

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