专利号:US-7968732-B1 优先权日:2010-09-07 标 题 :Process for the preparation of 5-benzyloxy-2-(4-benzyloxyphenyl)-3-methyl-1H-indole 发明人:DIVI MURALI KRISHNA PRASAD; RAO BOLINENI NAGESWARA; SURESH DANDU VENKATA 权利人:DIVIS LAB LTD 摘要:The present invention is related to a process for the preparation of 5-benzyloxy-2-(4-benzyloxyphenyl)-3-methyl-1H-Indole (formula-1, a useful intermediate for the synthesis of bazedoxifene) using 4-benzyloxy propiophenone and 4-benzyloxy phenyl hydrazine hydrochloride.
专利号:US-10844047-B2 优先权日:2018-06-21 标题:Process for the preparation of bazedoxifene 发明人:FERRARI MASSIMO; ZANI DANIELE DE; VEZZOSI STEFANO; BELOTTI PAOLO 权利人:ERREGIERRE SPA 摘要:The invention relates to a process for preparation of the compound 3-methyl-5-benzyloxy-2-(4-benzyloxyphenyl)-1H-indole 5, an intermediate for the synthesis of bazedoxifene and bazedoxifene acetate.
专利号:EP-1025077-B1 优先权日:1997-10-15 标题 :Novel aryloxy-alkyl-dialkylamines 发明人:RAVEENDRANATH PANOLIL; ZELDIS JOSEPH; VID GALINA; POTOSKI JOHN RICHARD; REN JIANXIN 权利人:WYETH CORP 摘要:The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having formula (I) wherein: R?1 and R2¿ are, independently, selected from H; C¿1?-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R?3, R4, R5, and R6¿ are independently selected from H, halogen, -NO¿2?, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, -CN, -O-R?1¿, -O-Ar, -S-R1, -S-Ar, -SO-R1, -SO-Ar, -SO¿2?-R?1, -SO¿2-Ar, -CO-R1, -CO-Ar, -CO¿2-R?1, or -CO¿2?-Ar; and Y is selected from a) the moiety (i) wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of -O-, -NH-, -N(C1C4 alkyl)-, -N=, and -S(O)n-.
专利号:US-6268504-B1 优先权日:1997-10-15 标题 :Aryloxy-alkyl-dialkylamines 发明人:RAVEENDRANATH PANOLIL; ZELDIS JOSEPH; VID GALINA; POTOSKI JOHN R; REN JIANXIN; IERA SILVIO 权利人:AMERICAN HOME PROD 摘要:The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula:wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, -NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, -CN, -O-R1, -O-Ar, -S-R1, -S-Ar, -SO-R1, -SO-Ar, -SO2-R1, -SO2-Ar, -CO-R1, -CO-Ar, -CO2-R1, or -CO2-Ar; and Y is selected from a) the moiety:wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of -O-, -NH-, -N(C1C4 alkyl)-, -N=, and -S(O)n-.
摘要:Stoltz, B. M.; Mohr, J. T., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 669. 摘要:Stoltz, B. M.; Mohr, J. T., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 662. 摘要:Wolf, C., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 880.