C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
530/5.04
C07F 9/28 (2006.01) C07F 9/30 (2006.01) C07F 9/38 (2006.01) C07K 5/06 (2006.01) C07K 5/08 (2006.01) C07K 5/10 (2006.01)
Patent
CA 1090785
ABSTRACT OF THE DISCLOSURE This invention relates to a process for the manufacture of peptide derivatives of the general formula Image (I) wherein n stands for 1, 2 or 3; R1 is methyl and R2 and R3 are methyl, isopropyl or isobutyl with the proviso that R3 is methyl when n is 1; R4 represents a hydroxy or methyl group; the con- figuration at the carbon atom designated as (a) is D; the con- figuration at the carbon atom designated as (b) is L; and the configuration at the carbon atom denoted as (c) is (R), and of pharmaceutically acceptable salts thereof, which process comprises (a) cleaving off the protecting group(s) present in a compound of the general formula Image (II) wherein n, R1, R and R3 have the significances given above; R40 represents a methyl group or R41; R41 represents a hydroxy group or lower alkoxy protecting group; R5 represents a hydrogen atom or a protecting group; and the configurations at the car- bon atoms designated as (a), (b) and (c) are as defined above, or (b) separating an (R,S)-diastereomeric compound corresponding to formula I into its diastereomers and isolating the (R)- diastereomer, and, if desired, converting an obtained compound of formula I into a pharmaceutically acceptable salt. me peptide derivatives of formula I potentiate the activity of D-cycloserine. In addition, they possess an antibacterial activity against organisms such as Escherichia coli, Klebsiella aerogenes, Streptococcus faecalisand Haemophilus influenzae.
278276
Atherton Frank R.
Hall Michael J.
Hassall Cedric H.
Lambert Robert W.
Ringrose Peter S.
Fetherstonhaugh & Co.
Hoffmann-La Roche Limited
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