Category: 1030377-21-9

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of intermediate 1.2 (4g) in MeCN (100ml_) were added (S)-1-Boc-2- hydroxymethylpiperazine (3.07g) and DIPEA (3.54ml_) at RT. The reaction mixture was stirred at 80C for 28h. After cooling down, the reaction mixture was diluted with EA and washed with water (2x) and brine. The aq. layers were extracted with EA. The combined org. layers were dried over MgS04, filtrated off and evaporated to dryness. The crude was purified by CC (Biotage, SNAP 340g, solvent A: Hep; solvent B: EA; gradient in %B: 30 over 3CV, 30 to 50 over 5CV, 50 over 3CV) to afford 4g of yellow foam. LC-MS (A): tR = 0.87min; [M+H]+: 426.0., 1030377-21-9

The synthetic route of 1030377-21-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; IDORSIA PHARMACEUTICALS LTD; CAROFF, Eva; MEYER, Emmanuel; (32 pag.)WO2018/11265; (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.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

a) To a solution of (R)-N-(l-(2,4-dichlorophenyl)ethyl)-5-fluoro-2-nitroaniline (prepared from Example 14 step a, 1.6 g, 4.9 mmol) and (5)-2-(hydroxymethyl)piperazine-l- carboxylic acid ?-butyl ester (0.99 g, 4.9 mmol) in anhydrous DMSO (10 mL) was added K2CO3 (1.88 g, 14.6 mmol). The reaction mixture was heated with stirring at 125 C for 2 h. After cooling to room temperature, the mixture was diluted with deionized water (10 mL) and stirred for 30 min. The aqueous layer was extracted with dichloromethane. The organic layer was dried (MgS04), filtered, and concentrated in vacuo. The crude oil was dried under vacuum to give the desired compound (1.9 g, 3.5 mmol, 73%).

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

Reference£º
Patent; CHEMOCENTRYX, INC.; LELETI, Manmohan Reddy; LI, Yandong; MALI, Venkat Reddy; POWERS, Jay; YANG, Ju; WO2013/82429; (2013); 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.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

To (S)-2-hydroxymethylpiperazine-1-carboxylic acid tert-butyl ester (950 mg) were added tetrahydrofuran (17 mL),3,5-dimethylpyridine-N-oxide (515 mg),N,N-diisopropylethylamine (2.8 mL) and bromotris(pyrrolidino)phosphonium hexafluorophosphate (2.67 g) and the mixture was stirred at room temperature for 5.5 hr. Water was added to the reaction mixture and the mixture was extracted with ethyl acetate. The solvent was evaporated and the obtained residue was purified by column chromatography (ethyl acetate:hexane)to give the title compound (640 mg). MS(ESI)m/z:322 (M+H)+

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

Reference£º
Patent; Mitsubishi Tanabe Pharma Corporation; ISHIBUCHI, Seigo; SARUTA, Kunio; HAMADA, Maiko; MATOBA, Nobuatsu; MATSUDAIRA, Tetsuji; SEKI, Maki; TARAO, Akiko; HONJO, Takashi; OGATA, Shingo; KAWATA, Atsushi; MOROKUMA, Kenji; FUJIE, Naoto; AOYAMA, Yukio; (251 pag.)EP3321256; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Into a 250-mL round-bottom flask purged and maintained with an inert atmosphere of nitrogen, was placed a solution of tert-butyl (2S)-2-(hydroxymethyl)piperazine-1-carboxylate (11.4 g, 52.7 mmol, 1.0 equiv) in DMSO (60 mL), 1,4-diiodobenzene (19.1 g, 59.9 mmol, 1.1 equiv), CuI (0.9 g, 5.2 mmol, 0.1 equiv), K2CO3 (14.5 g, 105.4mmol, 2.0 equiv), L-Proline (1.2 g, 10.4 mmol, 0.2 equiv). The resulting mixture was stirred for 12 hours at 90 C in an oil bath. The reaction was then quenched by the addition of 200 mL of water/ice. The resulting solution was extracted with ethyl acetate (200 mL x 2). The residue was applied onto a silica gel column eluting with ethyl acetate/petroleum ether (1:1). This resulted in 4.2 g (18.8%) of tert-butyl (2S)- 2-(hydroxymethyl)-4-(4-iodophenyl) piperazine-1-carboxylate as a solid. LC/MS (ESI) m/z: 419.05 [M+1] +., 1030377-21-9

The synthetic route of 1030377-21-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARVINAS OPERATIONS, INC.; YALE UNIVERSITY; CREW, Andrew P.; HORNBERGER, Keith R.; WANG, Jing; CREWS, Craig M.; JAIME-FIGUEROA, Saul; DONG, Hanqing; QIAN, Yimin; ZIMMERMAN, Kurt; (1451 pag.)WO2020/51564; (2020); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A vial was charged with 5-amino-3,6-dichloro-l ,2,4-triazine (589.6 mg, 3.57 mmol), triethylamine (1.5 mL, 10.76 mmol), (S)-tert-butyl 2-(hydroxymethyl)piperazine-l- carboxylate (890 mg, 3.99 mmol) in dioxane (12 mL). The mixture was heated at 95 C for 1.5 h using microwave. The mixture was cooled to room temperature and transferred into a flask with dichloromethane, concentrated to remove the solvents. The residue was mixed with saturated potassium carbonate, extracted with dichloromethane (3 x 40 mL). The combined organic solution was dried over anhydrous sodium sulfate, concentrated. The residue was separated with flash column chromatography on silica gel using 1-5% methanol in dichloromethane to afford the product (955.7 mg) in 78%. NMR (500 MHz, Chloroform- d) delta 5.30 (s, 2H), 4.69 (br, 1H), 4.45 (d, J= 12.3 Hz, 1H), 4.21 (s, IH), 3.88 (s, 1H), 3.52 (s, I 1H), 3.42 (s, 1H), 3.13 (d, J = 14.2 Hz, lH), 3.02 (t, J = 12.0 Hz, 1H), 2.93 (s, 1H), 1.43 (s, 9H). MS for C3H21CIN6O3: 345.2 (MH+)., 1030377-21-9

The synthetic route of 1030377-21-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics