1201901-80-5Relevant articles and documents
The scope and limitation of the regio- and enantioselective hydrolysis of aliphatic epoxides using Bacillus subtilis epoxide hydrolase, and exploration toward chirally differentiated tris(hydroxymethyl)methanol
Shimizu, Ken-Ichi,Sakamoto, Maki,Hamada, Manabu,Higashi, Toshinori,Sugai, Takeshi,Shoji, Mitsuru
experimental part, p. 2043 - 2049 (2010/10/19)
The substrate specificity of an engineered Bacillus subtilis epoxide hydrolase, which so far had shown high activity and enantioselectivity with 1-benzyloxymethyl-1-methyloxirane, has been studied by altering the methyl substituent into hydrogen, oxygen-containing functionalities, and unsaturated homologs. High enantioselectivity (E = 44) was observed with 1-benzyloxymethyl-1-vinyloxirane with a proper catalytic activity. The elaboration of the reaction conditions and work-up procedures enabled a preparative-scale kinetic resolution, to give (R)-2-benzyloxymethyl-3-butene-1, 2-diol and its antipodal (R)-epoxide in high ees.
Synthesis and evaluation of a new class of tertiary alcohol based BACE-1 inhibitors
Russo, Francesco,W?ngsell, Fredrik,S?vmarker, Jonas,Jacobsson, Micael,Larhed, Mats
experimental part, p. 10047 - 10059 (2010/02/28)
BACE-1 has emerged as one of the best characterized targets for future Alzheimer therapy. In accordance with the successful identification of masked inhibitors of HIV-1 protease, we envisioned that tert-alcohol containing transition-state mimicking struct
