专利号:EP-1476441-B1 优先权日:2002-01-23 标题 :A method of eliminating sulfone analog in the synthesis of pyridine-benzimidazole sulfoxides 发明人:UENSAL SERAFETTIN 权利人:ULKAR KIMYA SANAYII VE TICARET 摘要:Process for the preparation of pyridine-benzimidazole sulfinyl compounds such as Omeprazole, Lansoprozole and Pantoprozole of general formula (I), wherein the ring A may optionally be substituted, R1 is hydrogen or an N-protecting group, each of R2, R3 and R4 represent (1) a hydrogen atom, (2) alkyl group which may be substituted with halogen atom(s) or (3) an alkoxy group which may be optionally substituted with halogen atom(s) or alkoxy; or its salt. Sulphone analogs of the corresponding compounds as impurity are formed during oxidation of the precursor thioether of the compèound of formula (I). A process is provided for the elimination of sulphone analogs in contaminated products. The purification process comprises treatment of semi-pure benzimidazole derivatives with solid K2CO3 in alcohol medium at elevated temperatures.
专利号:WO-9840377-A1 优先权日:1997-03-07 标 题 :Process for the preparation of 2-[[(2-pyridinyl)methyl]sulfinyl]-1h-benzimidazoles and novel compounds of use for such purpose 发明人:CLAUSEN FINN PRIESS 权利人:BRISTOL MYERS SQUIBB CO; CLAUSEN FINN PRIESS 摘要:A process for the preparation of 2-[[2-pyridinyl)methyl]sulfinyl]-1-H-benzimidazole derivatives of general formula (I), wherein R2 represents H, OCH¿3?, OCHF2 or CF3; R?3¿ represents H, CH¿3? or OCH3; R?4¿ represents H, OCH¿3?, OCH2CF3, or halo, such as Cl, Br or F; and R?5¿ represents H, CH¿3? or OCH3, or salts thereof, comprising reducing a compound of general formula (II) or a salt thereof wherein R?2, R3, R4 and R5¿ are as defined above, in an alcoholic solvent, the reduction being carried out using a thiobisamine as reducing agent in the presence of a mineral acid, and, if desired, converting a compound obtained in free form into a salt thereof, or vice versa, and novel intermediates of formula (II) are described. The compounds of formula (I) are biologically active and/or may be of use as intermediates in the synthesis of biologically active compounds.
专利号:WO-9840378-A1 优先权日:1997-03-07 标题 :Process for the preparation of 2-[[(2-pyridinyl)methyl]sulfinyl]-1h-benzimidazoles and novel compounds of use for such purpose 发明人:CLAUSEN FINN PRIESS; MCCLUSKEY KLAUS KARL; PREIKSCHAT HERBERT FRITZ; PEDERSEN SOEREN BOLS 权利人:BRISTOL MYERS SQUIBB CO; CLAUSEN FINN PRIESS; MCCLUSKEY KLAUS KARL; PREIKSCHAT HERBERT FRITZ; PEDERSEN SOEREN BOLS 摘要:2-[[(2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole derivatives of general formula (V) wherein R2 represents H, OCH¿3?, OCHF2 or CF3, R?3¿ represents H, CH¿3? or OCH3, R?4¿ represents H, OCH¿3?, OCH2CF3, halo or nitro, R?5¿ represents H, CH¿3? or OCH3, and n is 0 or 1, or salts thereof, are prepared by a new process proceeding via novel intermediates of general formulae (I), (II), (III) and (Va) wherein R?1¿ represents branched or straight C¿1-8?-alkyl, C3-8-cycloalkyl, aryl, aralkyl having 1-8 C-atoms in the alkyl moiety, or a 5- or 6-membered heterocyclic group having one, two or three hetero atoms selected from nitrogen, sulfur and oxygen in the heterocyclic ring. The compounds of formula (V) are biologically active and/or may be used as intermediates in the synthesis of biologically active compounds.
专利号:US-9631181-B2 优先权日:2009-12-08 标 题 :Synthesis of prazole compounds 发明人:BONG YONG KOY; CLAY MICHAEL D; COLLIER STEVEN J; MIJTS BENJAMIN; VOGEL MICHAEL; ZHANG XIYUN; ZHU JUN; NAZOR JOVANA; SMITH DEREK J; SONG SHIWEI 权利人:CODEXIS INC 摘要:The present disclosure relates to non-naturally occurring monooxygenase polypeptides useful for preparing prazole compounds, polynucleotides encoding the polypeptides, and methods of using the polypeptides.
专利号:WO-03062223-A1 优先权日:2002-01-23 标题 :A method of eliminating sulfone analog in the synthesis of pyridine-benzimidazole sulfoxides
专利号:EP-0773940-B2 优先权日:1994-07-15 标 题:Process for synthesis of substituted sulphoxides