Downstream synthetic route of 129799-08-2

As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1:The mixture of methyl (¡À)-4-Boc-piperazine-2-carboxylate (CAS: 129799-08-2, 2.44 g, 0.01 mol), TEA (1.52 g, 0.015 mol) in DCM (10 mL) was added to a solution of (4-nitrophenyl) carbonochloridate (2.42 g, 0.012 mol) in DCM (10 mL). After 1 hour at rt, the organic layer was washed with water and saturated sodium bicarbonate solution, dried over sodium sulfate. After removal of solvent, the crude product 67-B was obtained and used in the next step without purification. MS: calc’d 410 (MH+), measured 410 (MH+)., 129799-08-2

As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference£º
Patent; HOFFMANN-LA ROCHE INC.; Guo, Lei; Hu, Taishan; Kou, Buyu; Lin, Xianfeng; Shen, Hong; Shi, Houguang; Yan, Shixiang; Zhang, Weixing; Zhang, Zhisen; Zhou, Mingwei; Zhu, Wei; US2015/252057; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate

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

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Benzyl carbonochloridate (6.43 mL, 45.03 mmol) was added to a solution of 1-tert-butyl 3-methyl piperazine-1,3-dicarboxylate (10 g, 40.94 mmol) and DIEA (14.30 mL, 81.87 mmol) in THF (100 mL) at 5C, and the mixture was stirred at room temperature for 14 hr. The reaction mixture was added to water and ethyl acetate. The organic layer was washed with aqueous ammonium chloride solution, dried over magnesium sulfate, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (solvent gradient; 5?20% ethyl acetate/hexane) to give 1-benzyl 4-tert-butyl 2-methyl piperazine-1,2,4-tricarboxylate (16.2 g, 42.8 mmol, 105%) as white crystals. 1H NMR (300 MHz, CDCl3):delta 1.44(9H,s), 2.63-3.48(3H,m), 3.74(3H,s), 4.11(2H,s), 4.44-4.86(2H,m), 5.08-5.26(2H,m), 7.22-7.42(5H,m).

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

Reference£º
Patent; Takeda Pharmaceutical Company Limited; YAMAMOTO, Satoshi; SHIRAI, Junya; ODA, Tsuneo; IMADA, Takashi; KONO, Mitsunori; SATO, Ayumu; TOMATA, Yoshihide; OCHIDA, Atsuko; ISHII, Naoki; SASAKI, Yusuke; FUKASE, Yoshiyuki; YUKAWA, Tomoya; FUKUMOTO, Shoji; (200 pag.)EP3192791; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 129799-08-2

As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

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.

To a stirred solution of 1-(tert-butyl) 3-methyl piperazine-1,3-dicarboxylate (250 mg, 1.023 mmol) in acetonitrile (8 mL) were added DIPEA (0.536 mL, 3.07 mmol) and 4,4′-(bromomethylene)bis(chlorobenzene) (485 mg, 1.535 mmol). The reaction mixture was heated up to 85 C over 10 min and was stirred for 16 h. The reaction mixture was concentrated under high vacuum to yield a brown gum. The crude compound was purified by ISCO (using 24 g silica gel column; using 8 % -12 % ethyl acetate/ petroleum ether) to yield 1-(tert-butyl) 3-methyl 4-(bis(4-chlorophenyl)methyl) piperazine-1,3-dicarboxylate (280 mg, 57.1 % yield) as a brown gum. LCMS: m/z = 481.2 (M+2H); rt 1.803 min; LC-MS Method: Column-KINETEX-XB-C18 (75 x 3 mm- 2.6 ^m); Mobile phase A: 10 mM ammonium formate in water: acetonitrile (98:2); Mobile phase B: 10 mM ammonium formate in water: acetonitrile (2:98); Gradient: 80 % B over 0.5 minute, 80-98% B over 2.5 minutes, flow rate 1.0 mL/min, then a 1 minute hold at 98% B flow rate 1.0 mL/min, 129799-08-2

As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; VELAPARTHI, Upender; CHUPAK, Louis S.; DARNE, Chetan Padmakar; DING, Min; GENTLES, Robert G.; HUANG, Yazhong; KAMBLE, Manjunatha Narayana Rao; MARTIN, Scott W.; MANNOORI, Raju; MCDONALD, Ivar M.; OLSON, Richard E.; RAHAMAN, Hasibur; JALAGAM, Prasada Rao; ROY, Saumya; TONUKUNURU, Gopikishan; VELAIAH, Sivasudar; WARRIER, Jayakumar Sankara; ZHENG, Xiaofan; TOKARSKI, John S.; DASGUPTA, Bireshwar; REDDY, Kotha Rathnakar; RAJA, Thiruvenkadam; (0 pag.)WO2020/6018; (2020); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics