FIELD: pharmacology.
SUBSTANCE: invention relates to a method for obtaining of a compound of formula or a salt thereof that can find application in the preparation of AKT inhibitors used to treat diseases such as cancer. The method includes asymmetrical reduction of a compound of formula or a salt thereof in the presence of a stereoselective reducing agent to form a compound of formula I. In formulas I and II, R1 and R2 are independently hydrogen, C1-C12 alkyl or an amino-protecting group. The invention also relates to compounds of formulas and , which are intermediate in the synthesis of the formula I compound. In formula VI, R1 is hydrogen, acetyl, trifluoroacetyl, phthalimide, benzyl, triphenylmethyl, benzylidenyl, t-butyloxycarbonyl, 9-fluorenylmethyloxycarbonyl or carbobenzyloxy; R2 is C1-C12 alkyl and R5 is hydrogen or C1-C12 alkyl. In formula VIb, R1 is hydrogen, acetyl, trifluoroacetyl, phthalimide, benzyl, triphenylmethyl, benzylidenyl, p-methoxybenzyl, t-butyloxycarbonyl, 9-fluorenylmethyloxycarbonyl or carbobenzyloxy.
EFFECT: increased application effeciency.
23 cl, 1 dwg, 2 ex
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Authors
Dates
2018-01-31—Published
2013-05-17—Filed