On January 28, 2010, Bury, Michael Jonathan; Cheung, Mui; Eidam, Hilary Schenck; Fox, Ryan Michael; Goodman, Krista; Manas, Eric Steven published a patent.SDS of cas: 85386-20-5 The title of the patent was Preparation of diazabicycloheptyl amino acid derivatives as transient receptor potential channel TRPV4 antagonists. And the patent contained the following:
Title compounds I [R1′ = (R1)i; i = 0-3; R1 = alkyl, alkoxy, CF3, halo, OCF3, CN, etc.; R2 = alkyl, cycloalkylmethyl, benzyl; R3 = (un)substituted pyrrolyl, pyrazolyl, tetrazolyl, isoquinolinyl,pyrimidinyl, etc.; ; G = (S,S)- or (R,R)-2,5-diazabicycloheptyl; X = a bond, CH2; Y = NH, N-alkyl, S; R5 = H, alkyl; and their pharmaceutically acceptable salts], were prepared Thus, a 5-step synthesis using 1,1-dimethylethyl (1S,4S)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylate, 3-methyl-N-[[(phenylmethyl)oxy]carbonyl]-L-valine, and 1H-indole-2-carboxylic acid gave II. Tested title compounds inhibited TRPV4 with IC50 in the range of 1 nM to 10 μM. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).SDS of cas: 85386-20-5
The Article related to diazabicycloheptylaminoacid preparation transient receptor potential channel trpv4 antagonist, overactive bladder pain cardiovascular disease arthritis treatment diazabicycloheptane preparation and other aspects.SDS of cas: 85386-20-5
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia