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Benzoicacid, 3-methyl-, 1,1-dimethylethyl ester synthesis

9synthesis methods
-

Yield:16537-19-2 97%

Reaction Conditions:

with hydrogen;palladium 10% on activated carbon in methanol;ethyl acetate; for 5 h;

Steps:

4.1 Example 4; Preparation of 2- I'd -Cyclohexyl-2- (2-fluoro-4- [3 -(4-hydroxyl-piperidine-1 -carbonyl)-benzyloxyj-phenyl) -1 ff-benzimidazole-5 -carbony l)-amino] -3 -(5 -hydroxy-1 ff-indol-3 -vl)-propionic acid hydrochloride (Compound 66); Scheme 7 above corresponds to the following procedures; 1. 3-Methyl-benzoic acid tert-butyl ester

[0128] 4-Bromo-3-methyl-benzole acid tert-butyl ester (0.39 g, 1.438mmol) was hydrogenated over 10% Pd-C (0.5 g) under H2 (50 psi) in EtOAc-MeOH (4:1,20 mL) for 5 h. After filtration through Celite, filtrate was evaporated to dryness. Yield:97%. MS (ESI) 193.28 (M + H+).

References:

WO2004/108687,2004,A2 Location in patent:Page 37