摘要:
The present invention relates to processes for selective sulfation of an aromatic hydroxyl group over an aliphatic hydroxyl group where both are present in the same molecule. This invention also relates to processes for selective sulfation of the aromatic hydroxyl group of equilin, equilenin, estradiol, estra(1,3,5-triene)-3,16,17-triol, dihydroequilenin or dihydroequilin. This invention further relates to alkali metal salts of dihydroequilenin sulfates, dihydroequilin sulfates, estradiol sulfates, and estriol sulfates, processes for making thereof, stable compositions comprising thereof, and the use thereof.
摘要:
Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.
摘要:
The present invention provides a process for the manufacture of an arylmethyl-sulfonylarene, R1CH2SO2R2, wherein R1 and R2 are each independently an optionally substituted phenyl or naphthyl group which process comprises reacting an arylmethylhalide, R1CH2-Hal wherein R1 is as defined hereinabove and Hal is Cl, Br or I with a sodium arylsulfinate R2SO2Na wherein R2 is as defined hereinabove in the presence of a base optionally in the presence of a solvent.Also provided is the use of the inventive process in the manufacture of a 3-arylsulfonylindazole 5-HT6 ligand.
摘要翻译:本发明提供了一种制备芳基甲基磺酰基芳烃R 1 CH 2 SO 2 R 2的方法,其中R 1和R 2各自独立地是任选取代的苯基或萘基,该方法包括使芳基甲基卤,R 1 CH 2 - Hal,其中R 1如上所定义,Hal是 Cl,Br或I与芳基亚磺酸钠R2SO2Na反应,其中R 2如上定义,在碱的存在下,任选地在溶剂存在下。 还提供本发明方法在制备3-芳基亚磺酰基吲唑5-HT 6配体中的用途。
摘要:
Processes are disclosed for preparing indolinone phenylaminopropanol derivatives, particularly chiral indolinone phenylaminopropanol derivatives of the general formula: The processes disclosed may be used to prepare, inter alia, 7-fluoro-1-[(1S, 2R)-1-(3-fluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one and 7-fluoro-1-[(1S, 2R)-1-(3,5-difluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one. Intermediates of the processes are also disclosed.
摘要:
Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.
摘要:
The present invention provides N′-(2-halobenzylidene)sulfonylhydrazides of formula I Compounds of formula I are useful for the manufacture of 1-arylsulfonylindazole 5-HT6 ligands.
摘要:
Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.