发明名称 Processes and intermediates for preparing 2-fluorothiophene derivatives.
摘要 PCT No. PCT/IB98/00304 Sec. 371 Date Jul. 26, 1999 Sec. 102(e) Date Jul. 26, 1999 PCT Filed Mar. 9, 1998 PCT Pub. No. WO98/45282 PCT Pub. Date Oct. 15, 1998A process for the preparation of the compound of the formula wherein R1 is OH, which comprises the steps of a) treating the compound of the formula with an inorganic fluoride, of the formula M2F wherein M2 is an alkali metal cation, at an elevated temperature in the presence of a compound of the formula R4P+Z- and a compound of the formula R5vic (COW)2 wherein R4 and R5 are each selected from optionally substituted (C6-C10)aryl and optionally substituted (C1-C6)alkyl, and W is halo; to form the compound of the formula; and b) i) treating the compound of the formula IV with an aqueous solution of a base, of the formula MOH, wherein M is an alkali metal cation, and ii) treating the product of step i) with a mineral acid. A compound of the formula wherein R1 is selected from the group consisting of, halo, R7O, R7COO and N(R8)2 wherein R7 is (C1-C6)alkyl or (C6-C10)aryl and each R8 is selected from hydrogen and R7 with the proviso that R7 is not methyl when R1 is R7O.
申请公布号 ZA9802850(B) 申请公布日期 1999.10.04
申请号 ZA19980002850 申请日期 1998.04.03
申请人 PFIZER INC. 发明人 ROBERT JAMES CHAMBERS;ANTHONY MARFAT
分类号 C07D333/38 主分类号 C07D333/38
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