{"id":1542,"date":"2021-01-22T02:31:41","date_gmt":"2021-01-21T18:31:41","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=1542"},"modified":"2021-01-22T02:31:41","modified_gmt":"2021-01-21T18:31:41","slug":"a-new-synthetic-route-of-863548-52-1-2","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=1542","title":{"rendered":"A new synthetic route of 863548-52-1"},"content":{"rendered":"

These common heterocyclic compound, 863548-52-1, name is (1-Methyl-1H-pyrazol-5-yl)methanamine, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. Quality Control of (1-Methyl-1H-pyrazol-5-yl)methanamine<\/a><\/p>\n

Example 241 Rac-4-((4bS,5R,6S,7S,7aR)-4b,5-dihydroxy-4-methoxy-6-((((1-methyl-1H-pyrazol-5-yl)methyl)amino)methyl)-7-phenyl-4b,5,6,7-tetrahydro-7aH-cyclopenta[4,5]furo[2,3-c]pyridin-7a-yl)benzonitrile (Cpd. No. 241F) (1493) Synthesis of rac-(4bS,5R,6R,7S,7aR)-7a-(4-bromophenyl)-4b,5-dihydroxy-4-methoxy-N-((1-methyl-1H-pyrazol-5-yl)methyl)-7-phenyl-4b,6,7,7a-tetrahydro-5H-cyclopenta[4,5]furo[2,3-c]pyridine-6-carboxamide. (Cpd. No. 241F) (1494) To the solution of rac-(4bS,5R,6R,7S,7aR)-7a-(4-bromophenyl)-4b,5-dihydroxy-4-methoxy-7-phenyl-4b,6,7,7a-tetrahydro-5H-cyclopenta[4,5]furo[2,3-c]pyridine-6-carboxylic acid (1, 1.00 g, 2.01 mmol) in N,N-dimethylformamide (5 mL) at 0 C., HATU (1.14 g, 3.01 mmol) and N,N-diisopropylethylamine (1.04 ml, 6.02 mmol) were added and the mixture was stirred for 5 min. (1-methyl-1H-pyrazol-5-yl)methanamine (2, 0.27 ml, 3.01 mmol) was added at the same temperature and the reaction was stirred for 16 h at room temperature. After completion, the reaction mixture was diluted with dichloromethane and washed with cold water. The organic layer was separated and dried over anhydrous sodium sulphate, filtered and concentrated to give crude product. The crude product was purified by silica gel (100-200 mesh size) column chromatography using 0-3% methanol in dichloromethane as eluent. The desired fractions were concentrated to afford rac-(4bS,5R,6R,7S,7aR)-7a-(4-bromophenyl)-4b,5-dihydroxy-4-methoxy-N-((1-methyl-1H-pyrazol-5-yl)methyl)-7-phenyl-4b,6,7,7a-tetrahydro-5H-cyclopenta[4,5]furo[2,3-c]pyridine-6-carboxamide (Cpd. No. 241F) as white solid. Yield: 0.85 g, 83%; MS (ESI) m\/z 591.41[M+1]+. 1H NMR (400 MHz, DMSO-d6); 1H NMR (400 MHz, DMSO-d6) 8.62 (t, J=5.2 Hz, 1H), 8.27 (s, 1H), 8.11 (s, 1H), 7.24 (d, J=9.0 Hz, 3H), 7.10-7.04 (m, 4H), 7.01-6.96 (m, 3H), 6.06 (s, 1H), 5.86 (s, 1H), 5.27 (bs, 1H), 4.63 (d, J=4.4 Hz, 1H), 4.40 (d, J=14.0 Hz, 1H), 4.35-4.21 (m, 2H), 3.97 (d, J=4.6 Hz, 1H), 3.91 (s, 3H), 3.61 (s, 3H).<\/p>\n

The synthetic route of (1-Methyl-1H-pyrazol-5-yl)methanamine has been constantly updated, and we look forward to future research findings.<\/p>\n","protected":false},"excerpt":{"rendered":"

The synthetic route of (1-Methyl-1H-pyrazol-5-yl)methanamine has been constantly updated, and we look forward to future research findings.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[320,131],"tags":[126],"class_list":["post-1542","post","type-post","status-publish","format-standard","hentry","category-863548-52-1","category-pyrazoles-derivatives","tag-m-w100-200"],"yoast_head":"\nA new synthetic route of 863548-52-1<\/title>\n<meta name=\"description\" content=\"These common heterocyclic compound, 863548-52-1, name is (1-Methyl-1H-pyrazol-5-yl)methanamine, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. 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