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US 6,686,471 B2Granted
Process and intermediates for growth hormone secretagogues
AssigneePfizer Inc.
InventorsCharles K. Chiu, David A. Griffith
Life of this patent
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Abstract
This invention relates to a process for preparing compounds of the Formula I, wherein R1, R2 and Pt are as defined in the specification, which are intermediates in the synthesis of certain growth hormone secretagogue compounds. This invention further relates to processes for preparing the growth hormone secretagogues. The invention also relates to the compound of Formula I wherein R1 is H, R2 is 2,2,2-trifluoromethyl and Pt is Boc.
Claims5
A compound of Formula VII,
- wherein
- Pt is an amine protecting group.
A process for preparing a compound of Formula XIII,
- comprising:
- (a) reacting piperazine-1,3-dicarboxylic acid 1-tert-butyl ester 3-(C1-C4)alkyl ester with a carbonyl equivalent and 2,2,2-trifluoroethylamine in the presence of a reaction inert solvent to form the compound of Formula XIV,
- (b) reacting said compound of Formula XIV with 2-picolyl-Z1, wherein Z1 is halo, methanesulfonyloxy or p-toluenesulfonyloxy, in the presence of a base and a reaction inert solvent to form the compound of Formula XV
- (c) reacting said compound of Formula XV with an acid in the presence a reaction inert solvent.
1 more element
Dependencies are inferred from the claim text.