摘要:
The present invention relates to biocatalytic asymmetric reduction for the preparation of 2-amino-[5-(1-hydroxy-2-hydroxy or halogen-ethyl)]-pyrazine derivatives of the formula wherein R is lower alkylcarbonyl or an amino protecting group and R1 is hydroxy or halogen. The compounds are key intermediates in the manufacture of a glucokinase activator.
摘要:
The present invention relates to biocatalytic asymmetric reduction for the preparation of 2-amino-[5-(1-hydroxy-2-hydroxy or halogen-ethyl)]-pyrazine derivatives of the formula wherein R is lower alkylcarbonyl or an amino protecting group and R1 is hydroxy or halogen. The compounds are key intermediates in the manufacture of a glucokinase activator.
摘要翻译:本发明涉及用于制备下式的2-氨基 - [5-(1-羟基-2-羟基或卤代 - 乙基)] - 吡嗪衍生物的生物催化不对称还原:其中R是低级烷基羰基或氨基保护基, R 1是羟基或卤素。 这些化合物是制造葡糖激酶活化剂的关键中间体。
摘要:
According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as novel synthesis routes for key intermediates used in those processes.
摘要:
A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.
摘要:
Provided is a crystalline IPA solvate of 2(R)-(3-Chloro-4-methanesulfonyl-phenyl)-3-((R)-3-oxo-cyclopentyl)-N-pyrazin-2-yl-propionamide as a glucokinase activator which increases insulin secretion in the treatment of, for example, type II diabetes.
摘要:
A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.
摘要:
According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
摘要:
Provided is a process for the preparation of 2(R)-(3-Chloro-4-methanesulfonyl-phenyl)-3-((R)-3-oxo-cyclopentyl)-N-pyrazin-2-yl-propionamide and its isopropanol solvate as a glucokinase activator which increases insulin secretion in the treatment of, for example, type II diabetes.
摘要:
A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.
摘要:
According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.