Process for the preparation of .alpha.-aminosubstituted...

C - Chemistry – Metallurgy – 07 – D

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C07D 223/16 (2006.01)

Patent

CA 2668823

The invention relates to use of a compound of formula Ib: (see formula Ib) in which; R is each independently H, A, -(CH2)r-OA, -(CH2)r-SA, cycloalkyl having 3 to 10 C atoms, -(CH2)s-cycloalkyl, fluoroalkyl having 1 to 3 C atoms, - (CH2)r-OAr, -(CH2)r-OHet, -(CH2)s-Ar, -(CH2)s-Het, NHA, NA2, -(CH2)s-NHA or -(CH2)s-NA2; R1 is each independently H, A, OA, SA, Hal, cycloalkyl having 3 to 10 C atoms, haloalkyl having 1 to 3 C atoms, haloalkoxy having 1 to 3 C atoms, haloalkylthio having 1 to 3 C atoms, -(CH2)t-OA, Het, -(CH2)t-Het, -(CH2)t-OAr, Ar, OAr, O- CH t- Ar, NO2, NHA, NA2, -(CH2)t-NHA, -(CH2)t-NA2, COOH, or CN; r is 2, 3 or 4; s is 1, 2 or 3; n is 2; t is 1, 2 or 3; A is alkyl having 1 to 8 C atoms; Ar is phenyl or naphthyl which are unsubstituted or mono- or disubstituted by A, OA or Hal; Hal is F, Cl, Br or I; Het is a saturated, partially or completely unsaturated mono- or bicyclic heterocyclic radical having 5 to 10 ring members, where 1 or 2 N and/or 1 or 2 S or O atoms can be present and the heterocyclic radical can be mono- or disubstituted by oxo, A, Hal, OH, OA, CF3, OCF3, NH2, NHA, NA2, COOH or COOA; in a nucleophilic substitution reaction.

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