公开(公告)号：US3487047A

公开(公告)日：1969-12-30

申请号：US3487047D

申请日：1968-03-18

Applicant: HOECHST AG

Inventor： WISSMANN HANS ,  SIEDEL WALTER ,  GEIGER ROLF

IPC: C07D333/16 ,  C08G16/04 ,  C08G5/18

CPC classification number: C07D333/16 ,  C08G16/04 ,  Y02P20/55

公开(公告)号：US3884897A

公开(公告)日：1975-05-20

申请号：US41031273

申请日：1973-10-29

Applicant: HOECHST AG

Inventor： GEIGER ROLF ,  WISSMANN HANS ,  LANGNER DIETRICH

IPC: C07K14/575 ,  A61K38/28 ,  A61P3/08 ,  A61P3/10 ,  C07C271/22 ,  C07K1/113 ,  C07K14/62 ,  C07C103/52 ,  C08H1/00

CPC classification number: C07K14/62 ,  C07C271/22 ,  Y02P20/55 ,  Y10S930/26

Abstract: BRIDGE BY Edman degradation. Compounds of the formula II.
A method for making insulin and certain derivatives thereof from a compound of the formula(I)

wherein Ac is an N-protective group removable by proton solvolysis X is hydrogen or an S-protective group, and n is 2 or 3, which comprises solvolyzing the Ac groups and dehydrogenating the -SX groups to S-S bonds to form a compound of the formula (II)
and then eliminating the

Abstract translation: 由式（I）的化合物制备胰岛素及其某些衍生物的方法，其中Ac是通过质子溶解分解可除去的N-保护基，X是氢或S-保护基，n是2或3，其包括溶剂分解 Ac基团并将-SX基团脱氢成SS键以形成式（II）的化合物，然后除去BRIDGE BY Edman降解。 式II的化合物。

公开(公告)号：US3457314A

公开(公告)日：1969-07-22

申请号：US3457314D

申请日：1964-07-28

Applicant: HOECHST AG

Inventor： SIEDEL WALTER ,  WISSMANN HANS

IPC: A01N35/02 ,  A61K31/11 ,  A61K31/43 ,  C07C45/63 ,  C07C47/24 ,  C07D213/20 ,  C07C47/48 ,  A61K27/00 ,  C07C45/00

CPC classification number: C07D213/20 ,  A61K31/43 ,  C07C45/63 ,  C07C47/24 ,  C07C205/44 ,  C07C49/24

公开(公告)号：US3920627A

公开(公告)日：1975-11-18

申请号：US46783274

申请日：1974-05-07

Applicant: HOECHST AG

Inventor： WISSMANN HANS ,  GEIGER ROLF ,  LINDNER ERNST ,  SCHOLKENS BERNWARD

IPC: C07K7/06 ,  A61K38/00 ,  A61P5/00 ,  C07C231/00 ,  C07K1/113 ,  C07K7/14 ,  C07C103/52 ,  A61K37/26

CPC classification number: C07K7/14 ,  A61K38/00 ,  Y02P20/55

Abstract: Peptides of the formula I X-Arg-Val-Tyr-Ile-His-Pro-Phegly-OH (I) in which X represents the radical of an aliphatic carboxylic acid of up to 5 carbon atoms or the phthalic acid radical, and Phegly-OH represents L-C-phenylglycine, and a process of preparing them by condensing the O-tert. butyl ester of compound I, in which tyrosine is protected by tert. butyl, and X represents hydrogen, with carboxylic acids of the formula X-OH, in which X has the first mentioned meaning, according to the condensation methods usually employed in peptide chemistry.

Abstract translation: 式I X-Arg-Val-Tyr-Ile-His-Pro-Phegly-OH（I）的肽，其中X表示至多5个碳原子的脂肪族羧酸基团或邻苯二甲酸基团，Phegly -OH表示LC-苯基甘氨酸，以及通过将O-叔丁基缩合制备它们的方法。 化合物I的丁酯，其中酪氨酸被叔保护。 丁基，X表示氢，根据肽化学中通常使用的缩合方法，具有式X-OH的羧酸，其中X具有第一个提及的含义。

公开(公告)号：US3872074A

公开(公告)日：1975-03-18

申请号：US26444172

申请日：1972-06-20

Applicant: HOECHST AG

Inventor： KONIG WOLFGANG ,  GEIGER ROLF ,  WISSMANN HANS

IPC: A61K38/00 ,  C07K1/10 ,  C07K5/06 ,  C07K14/625 ,  C07K14/695 ,  C07C103/52 ,  C07G7/00

CPC classification number: C07K5/06043 ,  A61K38/00 ,  C07K1/10 ,  C07K14/625 ,  C07K14/695

Abstract: A process for the manufacture of peptides by reacting a protected amino acid or a protected peptide ester with an optionally protected amino acid or a peptide having a free amino group, which may be bound to a polymer support, by adding a heterocyclic compound of the formula

D R A W I N G
WHEREIN X stands for the groups C O, C S or -N and X and N are members of a 5- or 6-membered heterocyclic ring optionally substituted and fused with a benzene nucleus and/or optionally containing 1 or 2 further hetero atoms, and the pK-value whereof lies between 3.7 and 4.2, as catalysts for the condensation.

Abstract translation: 通过将受保护的氨基酸或受保护的肽酯与任选保护的氨基酸或具有游离氨基的肽（其可以结合到聚合物载体）反应，通过加入式 其中X代表基团C = O，C = S或-N =且X和N是任选被取代并与苯核稠合的5或6元杂环的成员和/或任选地含有1或2个 杂原子，其pK值在3.7和4.2之间，作为缩合的催化剂。