99109-07-6Relevant articles and documents
Enantioselectivity of Pseudomonas cepacia lipase for the acetylation of 2-hydroxy carboxylic acid esters+
Sundholm, Oskari,Kanerva, Liisa T.
, p. 625 - 640 (2007/10/03)
Structurally different ethyl or methyl 2-hydroxy carboxylates were resolved by Pseudomonas cepacia lipase-catalysed acetylations with vinyl acetate in diethylether. One type of the alcoholic substrates (2-hydroxy-2-arylacetates and 2-hydroxy-3-arylpropinates) contained a HO-group at the stereocentre. These compounds were resolved with high enantioselectivity (ee 91 → 99) at ca. 50% conversion. The other alcoholic substrates ((threo-2-hydroxy-3-methylbutyrate and threo- or erythro-2-hydroxy-3-aryl-3-arylthio(or aryloxy)propionates) with two stereocentres generally resulted in enantiopure products and the reactions stopped at 50 % conversion.
Process for preparing 1,5-benzothiazepine derivatives
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, (2008/06/13)
There is disclosed a process for preparing 1,5-benzothiazepine derivatives of the formula: STR1 wherein R1 is a lower alkyl group, or a salt thereof which comprises subjecting a propionate derivatives of the formula: STR2 wherein R2 is an ester residue and R1 is the same as defined above, to intramolecular cyclization in the presence of a sulfonic acid compound of the formula: wherein R3 is a lower alkyl group or a substituted or unsubstituted phenyl group, in a non-halogenated organic solvent and, if desired, converting the product to a salt thereof.
Process for the resolution of intermediates useful in the preparation of 1,5-benzothiazepines
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, (2008/06/13)
A process for the resolution of amminoesters of the formula wherein R1 and R3 have the meanings reported in the specification, by tartaric acid and analogs thereof, is described. The compounds of formula IV-A are intermediates useful in the preparation of optically active 2-(4-methoxyphenyl)-1,5-benzothi-azepin-4(5H)ones.