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【结 构 式】

【分子编号】62963

【品名】2-thiophenylboronic acid

【CA登记号】

【 分 子 式 】C4H5BO2S

【 分 子 量 】127.9595

【元素组成】C 37.55% H 3.94% B 8.45% O 25.01% S 25.06%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(XV)

Bromination of 5-aminopyrazole (XI) with Br2 in AcOH gives 4-bromo-5-aminopyrazole (XII), which is cyclized with N-[3-[3-(dimethylamino)-2-propenoyl]phen-yl]-N-methylacetamide (X) in AcOH to yield the 3-bromo-pyrazolo[1,5-a]pyrimidine derivative (XIII). Finally, this compound can be condensed with either 2-thienylcarbonyl chloride (XIV) by means of Zn or Mg or with 2-thienylboronic acid (XV) and CO by means of a Pd(0) catalyst.

1 Sorbera, L.A.; Castaner, J.; Martin, L.; Indiplon. Drugs Fut 2003, 28, 8, 739.
2 Wilcoxen, K.M.; Gross, R.S. (Neurocrine Biosciences Inc.); Synthesis of substd. pyrazolopyrimidines. WO 0110868 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(X) 59947 N-{3-[(E)-3-(dimethylamino)-2-propenoyl]phenyl}-N-methylacetamide C14H18N2O2 详情 详情
(XI) 56012 1H-pyrazol-5-amine; 1H-pyrazol-5-ylamine 916420-28-5 C3H5N3 详情 详情
(XII) 62961 4-bromo-1H-pyrazol-5-ylamine; 4-bromo-1H-pyrazol-5-amine C3H4BrN3 详情 详情
(XIII) 62962 N-[3-(3-bromopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-methylacetamide C15H13BrN4O 详情 详情
(XIV) 14103 2-Thiophenecarbonyl chloride 5271-67-0 C5H3ClOS 详情 详情
(XV) 62963 2-thiophenylboronic acid C4H5BO2S 详情 详情
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