Title:
PRODUCTION OF HALOGENATED ALPHA-AMINOKETONE AND ALPHA-AMINOALCOHOL
Document Type and Number:
Japanese Patent JP3599855
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To provide a process for producing a halogenated α-aminoketone and α-aminoalcohol useful as an intermediate for a pharmacologically active compound, especially a compound suitable for treatment of virus infectious disease.
SOLUTION: An ester of formula II (R3 is an alkyl) is reacted with a lower alkyllithium (e.g. hexyllithium) or an organic chlorosilane of the formula ClSi (R4, R5, R6) (R4 to R6 are each independently a lower alkyl or phenyl) to provide an intermediate of silyl-protected compound, and further reacting the intermediate in the presence of methane dihalide (e.g. bromochloromethane) or the like to provide the objective compound of formula I (X is a halogen; one of Q1 and Q2 is H and the other is hydroxy, or Q1 and Q2 form oxo; R1 is an amino protective group; R2 is H or a characterizing group of an aminocarboxylic acid), e.g. methyl (S) 2 methoxycarbonylamino-3-phenylpropionate in the process for producing a halogenated α-aminoketone and α-aminoalcohol.
Inventors:
Hans Hilpert
Application Number:
JP26204495A
Publication Date:
December 08, 2004
Filing Date:
September 18, 1995
Export Citation:
Assignee:
F. HOFFMANN-LA ROCHE AKTIENGESELLSCHAFT
International Classes:
C07B61/00; C07C269/06; C07C271/16; C07C271/18; C07C319/20; C07C323/43; (IPC1-7): C07C269/06; C07C271/16; C07C271/18; C07C319/20; C07C323/43
Domestic Patent References:
| JP3255076A | ||||
| JP8099959A |
Other References:
J.Med.Chem.,1990年,Vol.33,pp1285-1288
Attorney, Agent or Firm:
Heikichi Odashima
Previous Patent: FACE FITTING IMAGE DISPLAY DEVICE FOR MEDICAL USE
Next Patent: PNEUMATIC TRANSPORT DEVICE
Next Patent: PNEUMATIC TRANSPORT DEVICE