Simple exploration of 1169563-99-8

The synthetic route of 1169563-99-8 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1169563-99-8,tert-Butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

4- (5-amino -1H- pyrazol-3-yl) piperidine-1-carboxylic acid tert- butyl (compound described in WO2011 / 045344 pamphlet, 13.5 g, 50.7 mmol) ethyl acetate (60 mL) to the solution under cooling with ice, it was added dropwise hydrochloric acid (4M in dioxane, 31.7mL, 127mmol), followed by stirring at room temperature for 3 hours.After stirring for 10 minutes by adding ethyl acetate (40 mL) to the reaction solution, and collected by filtration and the resulting precipitate to give the title compound (12.5 g, yield: 100%) was obtained., 1169563-99-8

The synthetic route of 1169563-99-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Daiichi Sankyo company limited; Sato, Rie; Kobayashi, Katsuhiro; Kaneko, Toshio; (188 pag.)JP2015/113323; (2015); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

New learning discoveries about 1169563-99-8

1169563-99-8, 1169563-99-8 tert-Butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate 49761279, apiperidines compound, is more and more widely used in various fields.

1169563-99-8, tert-Butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 18 – Preparation of Compound 15 The synthesis of Compound 15 followed the procedure of General Procedure 4 following: Compound 14 Compound 15 To a solution of tert-butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate (Compound 14, 3.0 g, 11.3 mmol, 1.0 eq) in methanol (30 mL) was added acetic acid (0.67 mL, 11.3 mmol, 1.0 eq), followed by 5-chlorothiophene-2-carbaldehyde (1.81 g, 12.4 mmol, 1.1 eq) portionwise. The reaction was stirred for 2 hours at room temperature. To the reaction mixture was then added sodium cyanoborohydride (1.42 g, 22.6 mmol, 1.5 eq) portionwise over a period of 45 minutes. The reaction mixture was stirred for a further 3 hours. After reaction completion, the reaction mixture was concentrated under reduced pressure, and the residue was poured into stirred ice cold water and extracted with ethyl acetate. The organic layer was dried over sodium sulfate, filtered and evaporated under reduced pressure. The residue was purified by column chromatography using neutral silica gel, eluting with 5-10% methanol in dichloromethane, yielding tert-butyl 4-(5-(((5-chlorothiophen-2-yl)methyl)amino)- 1H-pyrazol-3-yl)piperidine-1-carboxylate (Compound 15, 3.0 g, yield: 68%) m/z[M+H]+ 396.14 1H NMR (DMSO-d6, 400 MHz) delta 11.34 (1H, s), 6.87-6.94 (1H, q), 6.834-6.843 (1H, q), 5.68 (1H, s), 4.275-4.288 (1H, s), 3.945-3.975 (2H, d),2.786- 2.796 (2H, d), 2.623-2.681(1H, d), 1.725-1.995 (2H, d), 1.402-1.559 (12H, m) ppm.

1169563-99-8, 1169563-99-8 tert-Butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate 49761279, apiperidines compound, is more and more widely used in various fields.

Reference:
Patent; VERSEON CORPORATION; SHORT, Kevin Michael; ESTIARTE-MARTINEZ, Maria de los Angeles; KITA, David Ben; SHIAU, Timothy Philip; (340 pag.)WO2016/138532; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Analyzing the synthesis route of 1169563-99-8

As the paragraph descriping shows that 1169563-99-8 is playing an increasingly important role.

1169563-99-8, tert-Butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of tert-butyl 4-(5-amino-lH-pyrazol-3-yl)piperidine-l-carboxylate (300 mg, 1.126 ramol), 2-bromo-5-cyclopropylpyridine (234mg, 1.183mmol), copper(I) iodide (21.45mg, 0.1 13mmol), (lS,2S)-NN2-dime ylcyclohexane-l,2-diamine (16.02 mg, 0.113 mmol), and cesium carbonate (734mg, 2.253 mmol), DMSO (3 rnL), was purged with N2 for 30 min. The mixture was heated to 130 C in a sealed tube for 15 h. The mixture was cooled to rt. and water (30 mL) was added. The mixture was extracted with EtOAc (3 x 30 mL). The combined organic extracts were dried (MgS04) and concentrated in vacuo. The residue was purified by silica gel chromatography, eiuting with a solvent gradient of 0 to 40 % EtOAc in hexanes to give the product as a white solid. 1H NMR (400 MHz, CDC13) delta 8.03 (m, 1H), 7.74 (m, 1H), 7.32 (m, 1H), 5.88 (bs, 2H), 5.26 (s, 1H), 4.10 (m, 2H), 2.79 (m, 2H), 2.67 (m, 1H), 1.88-1.79 (ra, 3H), 1.61-1.54 (m, 2H), 1.42 (s, 9H), 1.20(t, J- 7.2 Hz, 1H), 0.94 (m, 2H), 0.63 (m, 2H)., 1169563-99-8

As the paragraph descriping shows that 1169563-99-8 is playing an increasingly important role.

Reference:
Patent; MERCK SHARP & DOHME CORP.; MCELROY, William, T.; LI, Guoqing; HO, Ginny Dai; TAN, Zheng; PALIWAL, Sunil; SEGANISH, William Michael; TULSHIAN, Deen; LAMPE, John; METHOT, Joey, L.; ZHOU, Hua; ALTMAN, Michael, D.; ZHU, Liang; WO2012/129258; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem