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US 10,988,446 B2Granted
Concise process for preparing 3-pyrrolidine carboxylic acid derivatives
AssigneeOkinawa Institute of Science and Technology School Corporation
InventorsFujie Tanaka, Feng Yin
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Abstract
The present invention relates to a process for preparing 3-pyrrolidine carboxylic acid derivatives, and particularly a simple process for preparing 5-substituted 3-pyrrolidine carboxylic acid derivatives. In addition, the present invention relates to a novel pyrrolidine carboxylic acid derivative, its manufacture, pharmaceutical compositions containing it and its use as a catalyst.
Claims2
A process for preparing compound of formula I′:
- wherein
- R1 and R2 are each independently hydrogen, C1-7-alkyl, C3-7-cycloalkyl, halo-C1-7-alkyl, C1-7-alkoxy-C1-7-alkyl, aryl-C1-7-alkyl, or heteroaryl-C1-7-alkyl;
- or
- R1 and R2 together form —(CH2)n—, and n is 2 to 6;
- R3 is hydrogen, C1-7-alkyl, C3-7-cycloalkyl, halo-C1-7-alkyl, C1-7-alkoxy-C1-7-alkyl, aryl-C1-7-alkyl, or heteroaryl-C1-7-alkyl;
- R4 is hydrogen, C1-7-alkyl, C3-7-cycloalkyl, halo-C1-7-alkyl, C1-7-alkoxy-C1-7-alkyl, aryl-C1-7-alkyl, or heteroaryl-C1-7-alkyl;
- and
- R5 is hydrogen, C1-7-alkyl, C3-7-cycloalkyl, halo-C1-7-alkyl, C1-7-alkoxy-C1-7-alkyl, aryl-C1-7-alkyl, or heteroaryl-C1-7-alkyl;
- or a pharmaceutically acceptable salt thereof, which process comprises
- step A:
- reacting compound of formula II:
- wherein R1 and R2 are as defined above, with compound of formula III:
- wherein R3, R4 and R5 are as defined above, in the presence of at least one of compound X which is selected from the group consisting of:
- to obtain compound of formula IV:
- wherein R1, R2, R3, R4, and R5 are as defined above,
- step B:
- reacting compound of formula IV with a reductant to obtain compound of formula I′.
14 more elements
Dependencies are inferred from the claim text.