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    • 10. 发明专利
    • DE2147799B2
    • 1981-02-26
    • DE2147799
    • 1971-09-24
    • N.V. ORGANON, OSS (NIEDERLANDE)
    • WIED, DAVID DE, PROF. DR., BILTHOVEN (NIEDERLANDE)
    • C07K7/16A61K37/02
    • 1342803 Peptides ORGANON LABORATORIES Ltd 14 Sept 1971 [26 Sept 1970] 42869/71 Heading C2C [Also in Division A5] The following reaction sequences are disclosed (Al) Z-Pro-OH. (Z is benzyloxycarbonyl) and H - Lys(tosyl) - OCH 3 .HCl give Z - Pro- Lys(tosyl) - OCH 3 . (A2) This product is hydrogenated in HCl to H-Pro-Lys(tosyl)- OCH 3 .HCl. (A3) This product is reacted with Z - Glu(NH 2 ) - Asp(NH 2 ) - Cys(benzyl) - OH to give Z - Gln - Asn - Cys(benzyl - Pro - Lys- (tosyl)-OCH 3 (A4) This product is saponified to give Z - Gln - Asn - Cys(benzyl) - Pro - Lys (tosyl)-OH. (A5. 1) This product is hydrogenated to H-Gln-Asn-Cys(benzyl)-Pro-Lys(tosyl)- OH. (A5. 2) Z - Gln . Asn - Cys(benzyl) - Pro- Lys(tosyl)-OCH 3 is hydrogenated to H-Gln- Asn - Cys(benzyl) - Pro - Lys(tosyl) - OCH3. Example I Z.Cys(benzyl)-Tyr-Phe-N 2 H 3 is reacted with H - Gln - Asn . Cys(benzyl) - Pro- Lys(tosyl)-OH.HCl and all protecting groups removed to give Similar reactions are also disclosed in which lysine is replaced by arginine. (B1-B5 and Example II). Hydrochloride, phosphate and maleates of the final products are prepared.