Intermediates for the preparation of 1-(phenyl)-1-

专利名称：Intermediates for the preparation of 1-(phenyl)-1-hydroxy-2-amino- 3-fluoropropane derivatives

发明人：Giancarlo Jommi,Dario Chiarino申请号：US07/162247申请日：19880229公开号：US05105009A公开日：19920414

摘要：Intermediates of Formula ##STR1## where R is a methylthio, methylsulfoxy,methylsulfonyl or a nitro group; and

X1 is hydrogen, 1-6 C alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl, phenyl or phenylalkyl(1-6C), where the phenyl ring may be substituted by one or two halogen, 1-3 C alkyl, 1-3 Calkoxy or nitro; or

X1 together with X2 is an oxygen atom or an alkylene having from two to five Carbonatoms; or

X1 together with X2 and R4 is a chain of formula ##STR2## where p is 3 or 4 and q is 1or 2; and X2 is hydrogen, 1-6 C alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl or phenyl which maybe substituted by one or two halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; or

X2 together with R4 is ##STR3## where n is 1 or 2; m is 0 or 1; X is hydrogen, halogen,1-3 C alkyl, 1-3 C alkoxy or nitro; and

X3 is hydrogen or --CO--R4 where R4 is hydrogen, 1-6 alkyl, 1-6 C haloalkyl, 3-6 Ccycloalkyl, phenylalkyl(1-6C) or phenyl where the phenyl ring may be substituted by one

or two halogen, 1-3 alkyl, 1-3 alkoxy or nitro; and

X4 is --OH, fluorine, OCOAlkyl(1-4C), --O--trialkyl(1-6C)silyl, --O--tetrahydropyranyl, --O-- tetrahydrofuranyl or --O--SO.sub.2 R.sub.6 where R6 is methyl, trifluoromethyl,phenyl or p-methyl-phenylprovided, however, that X4 is not OH when R is a nitro group;

for the preparation of 1- (phenyl)-1-hydroxy-2-amino-3-fluoropropane derivatives.

申请人：ZAMBON S.P.A.

代理机构：Cushman, Darby & Cushman

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