公开(公告)号：US3772264A

公开(公告)日：1973-11-13

申请号：US3772264D

申请日：1971-09-17

Applicant: HOFFMANN LA ROCHE

Inventor： BAYER E ,  MUTTER M ,  GILLESSEN D ,  KUENZI H ,  STUDER R

IPC: C07C233/09 ,  C07K1/04 ,  C07K5/103 ,  C07C103/52 ,  C07G7/00 ,  C08H1/00

CPC classification number: C07K1/042 ,  C07K5/1005

Abstract: PEPTIDES ARE PREPARED IN A HOMOGENEOUS SYSTEM BY COUPLING A FIRST AMINO ACID TO A SOLUBLE POLYMER SUPPORT AND THEREAFTER COUPLING ADDITIONAL AMINO ACIDS IN DESIRED SEQUENCE UNTIL THE ULTIMATE PEPTIDE IS OBTAINED. REAGENTS USED IN THE INTERMEDIATE STEPS ARE READILY SEPARATED FROM THE COUPLED POLYMER-AMINO ACID CHAIN BY SELECTIVE FILTRATION TECHNIQUES. IN THE FINAL STEP THE DESIRED PEPTIDE IS CLEAVED FROM THE POLYMER SUPPORT AND SEPARATED FROM THE SOLUBLE POLYMER BY USE OF ULTRAFILTRATION.

公开(公告)号：SE398347B

公开(公告)日：1977-12-19

申请号：SE1213571

申请日：1971-09-24

Applicant: HOFFMANN LA ROCHE

Inventor： GILLESSEN D ,  KUNZI H ,  STUDER R ,  BAYER E ,  MUTTER M

IPC: C07C233/09 ,  C07K1/04 ,  C07K5/103 ,  C07C103/52

Abstract: 1310656 Peptide process F HOFFMANNLA ROCHE & CO AG 24 Sept 1971 [26 Sept 1970] 44701/71 Heading C2C [Also in Division C3] In a peptide process an amino acid which is linked via an ester or amide bond to a polymer which is soluble in water and/or an organic solvent is stepwise coupled in a homogeneous phase with further amino acids and the polymer removed from the peptide. Polymers have mol. wts. of up to 100,000 and are preferably polyethylene glycol optionally esterified with citric acid or a copolymerizate of vinyl pyrrolidone and acrylic acid #-hydroxyethylacrylate or of acrylamide and vinyl acetate in which the ester groups are partially saponified at least, or a copolymerizate of polyethylene glycol and succinic acid. In the process lower molecular coupling reagents are removed by dialysis, membrane filtration, column chromatography or countercurrent distribution and the polymer is removed from the peptide by treatment with dilute alkali hydroxide. Maleic acid di-(p-nitrophenyl) ester is prepared from the acid and phenol in the presence of dicyclohexylcarbodiimide and then with HI to give mono iodo succinic acid di-(p-nitrophenyl) ester.