公开(公告)号：JP2008013568A

公开(公告)日：2008-01-24

申请号：JP2007175902

申请日：2007-07-04

Applicant: Degussa Gmbh ,  デグサ ゲーエムベーハーDegussa GmbH

Inventor： KNAUP GUENTER

IPC: C07C231/12 ,  C07B57/00 ,  C07C53/134 ,  C07C237/04 ,  C07C271/22 ,  C07D301/03 ,  C07D303/48

CPC classification number: C07D303/48 ,  C07C231/12 ,  C07C231/20 ,  C07C237/04 ,  C07C271/22 ,  C07C2601/02

Abstract: PROBLEM TO BE SOLVED: To provide a method for producing an enantiomerically pure 3-amino-2-hydroxamide starting from an easily available starting material taking consideration of the prior art, and easily practicable on an industrial scale without imposing particular requirement on industrial apparatuses. SOLUTION: The objective compound is produced from an epoxy-carboxylic acid amide expressed by formula 2 by reacting the acid amide with ammonia or other amine. COPYRIGHT: (C)2008,JPO&INPIT

Abstract translation: 待解决的问题：提供从考虑现有技术的容易获得的原料开始制备对映异构体纯的3-氨基-2-羟基酰胺的方法，并且在工业规模上容易实用，而不特别要求 工业设备。 解决方案：通过使酰胺与氨或其它胺反应，由式2表示的环氧 - 羧酸酰胺制备目标化合物。 版权所有（C）2008，JPO＆INPIT

公开(公告)号：JP2000219683A

公开(公告)日：2000-08-08

申请号：JP2000020674

申请日：2000-01-28

Applicant: DEGUSSA

Inventor： HELENE COLLET ,  MION LOUIS ,  JACQUES TAYAADE ,  AUGUSTE KONMEIRASU ,  ERNST ROBERT BAARENSHEE ,  KNAUP GUENTER

IPC: C07B51/00 ,  C07C209/62 ,  C07C211/27 ,  C07C227/20 ,  C07C229/26 ,  C07D263/44 ,  C07K1/12

Abstract: PROBLEM TO BE SOLVED: To provide a simple and widely applicable method of decarbamoylating a compound having a specific N-carbamoyl protecting group with nitrogen oxide. SOLUTION: This is a method for decarbamoylating of a compound having an N-carbamoyl protecting group of the formula (R1 is a 1-8C alkyl, a 2-8C alkenyl or the like; and R2 is H or R1) with a nitrogen oxide of the formula: NxOy [(x) is 1 or 2; and (y) is 1-3]. The reaction is advantageously performed in a fluidized bed as a gas-solid reaction. As a compound of the formula, a peptide having an N-carbamoyl protecting group or an amino acid having an N-carbamoyl protecting group is preferably used and use of an N,N'-dicarbamoyl protecting diaminocarboxylic acid or an N,N'-dicarbamoyl-lysine is preferably used. Preferably, 0.5-50 mass % of water and 0.01-20 mass % of an acid (e.g. acetic acid) based on a using solid are added to the reaction system at from -20 deg.C to 150 deg.C.

公开(公告)号：JPH11349567A

公开(公告)日：1999-12-21

申请号：JP13876399

申请日：1999-05-19

Applicant: DEGUSSA

Inventor： DRAUZ KARLHEINZ ,  KNAUP GUENTER ,  SCHWARM MICHAEL

IPC: C07C229/22 ,  C07C237/06 ,  C07C237/08 ,  C07C237/22 ,  C07C255/60 ,  C07C271/22 ,  C07C305/08 ,  C07C309/70 ,  C07D207/26 ,  C07D207/273

Abstract: PROBLEM TO BE SOLVED: To obtain the subject compound in high yield by cyclization of a specific compound having a halogen or sulfonic ester group. SOLUTION: This compound of formula II is obtained by cyclization of a compound of formula I [R is H, a (substituted) 1-8C alkyl, p-cyanophenyl, p-carbamoyl or the like; R is H, a (substituted) 2-8C alkenyl or the like; R is H, ClCO, formyl, benzyloxycarbonyl or the like; X is a halogen or sulfonic ester group] pref. using a base (e.g. sodium hydroxide) at -20 to 100 deg.C. By the way, the compound of formula I is prepared by reaction of a compound of formula III pref. in a solvent such as toluene or methyl-isobutyl ketone in the presence of a base (e.g. mesyl chloride).

公开(公告)号：JP2000086626A

公开(公告)日：2000-03-28

申请号：JP25453699

申请日：1999-09-08

Applicant: DEGUSSA

Inventor： DRAUZ KARLHEINZ ,  KLEMENT INGO DR ,  KNAUP GUENTER

IPC: C07C321/14 ,  C07C323/60 ,  C07C381/12 ,  C07D207/26 ,  C07D207/273

Abstract: PROBLEM TO BE SOLVED: To obtain a γ-lactam useful as an intermediate for producing physiologically actively acting substances in an industrial scale by cyclizing a specific derivative, while avoiding the employment of a dangerous substance and an expensive reagent as much as possible. SOLUTION: This method for producing a γ-lactam of formula II comprises cyclizing a derivative of formula I [R1, R2 are each H, a (substituted) 1-8C alkyl, a 2-8C alkenyl, a 2-8C alkynyl or the like; R3 is H, a 1-8C acyl, a C- bonded amino acid group or the like; Y is a 1-4C alkyl, a 1-8C (substituted) alkylene or the like]. The reaction is preferably carried out under a basic condition such as potassium hydroxide or potassium hydroxide in a polar protonic solvent such as methanol in a temperature range of 0-150 deg.C.

公开(公告)号：WO0183423A3

公开(公告)日：2002-02-21

申请号：PCT/EP0104085

申请日：2001-04-10

Applicant: DEGUSSA

Inventor： KNAUP GUENTER

IPC: C07D233/78 ,  C07C229/08 ,  C07C229/12 ,  C07C229/22 ,  C07C229/26 ,  C07C229/30 ,  C07C231/06 ,  C07C233/47 ,  C07C233/91 ,  C07C255/24 ,  C07C255/30 ,  C07D233/72 ,  C07D487/08

CPC classification number: C07C229/08 ,  C07C229/12 ,  C07C229/26 ,  C07C229/30 ,  C07C233/47 ,  C07C233/91 ,  C07C255/24

Abstract: The present invention is directed towards compounds of general formula (I). (I) are important intermediates for the preparation of pharmaceuticals. Further intermediates, process for the preparation of formula (I) and use thereof.

Abstract translation: 本发明涉及通式（I）的化合物。 （I）是制备药物的重要中间体。 其它中间体，式（I）的制备方法及其用途。

公开(公告)号：DE102005012771A1

公开(公告)日：2006-09-21

申请号：DE102005012771

申请日：2005-03-19

Applicant: DEGUSSA

Inventor： KNAUP GUENTER ,  LATINOVIC MILAN

IPC: C07D209/52 ,  C07C271/06

Abstract: The present invention is aimed at a process for the preparation of compounds of the general formula (I). The objective process is in this case based on the Michael reaction of compounds of the general formula (III) with compounds of the general formula (IV), with subsequent hydrogenation and cyclization of the intermediates of the formula (II) obtained.

公开(公告)号：NO20025004D0

公开(公告)日：2002-10-17

申请号：NO20025004

申请日：2002-10-17

Applicant: DEGUSSA

Inventor： DRAUZ KARLHEINZ ,  KNAUP GUENTER

IPC: C07D241/08 ,  C07K5/06 ,  C07K5/068 ,  C07K5/12 ,  C07D

公开(公告)号：DE59602002D1

公开(公告)日：1999-07-01

申请号：DE59602002

申请日：1996-01-31

Applicant: DEGUSSA

Inventor： DRAUZ KARLHEINZ ,  KNAUP GUENTER ,  RETZOW STEFAN ,  SCHWARM MICHAEL ,  WECKBECKER CHRISTOPH

IPC: C07K5/06 ,  C07K5/072 ,  C07K5/075

Abstract: PCT No. PCT/EP96/00393 Sec. 371 Date Nov. 21, 1997 Sec. 102(e) Date Nov. 21, 1997 PCT Filed Jan. 31, 1996 PCT Pub. No. WO96/26213 PCT Pub. Date Aug. 29, 1996The invention concerns a method of producing L-aspartyl-D-alanine-N-(thietane-3-yl) amides of general formula I by reacting D-alanine-thietane amides of general formula II with oxazolidinone compounds of general formula III in an inert organic solvent, wherein R1 stands for H or a selectively separable protective group, R2-R5 independently of one another, are identical or different and stand for H or linear or branched C1-C4-alkyl, and R6 and R7, independently of each other, are identical or different and stand for H, linear or branched C1-C4-alkyl, aryl or a group which activates the carbonyl group. (I) (II) (III)

公开(公告)号：ZA961344B

公开(公告)日：1996-08-26

申请号：ZA961344

申请日：1996-02-20

Applicant: DEGUSSA

Inventor： KNAUP GUENTER ,  RETZOW STEFAN ,  WECKBECKER CHRISTOPH

IPC: C07D331/04 ,  C07D

公开(公告)号：ZA9601344B

公开(公告)日：1996-08-26

申请号：ZA9601344

申请日：1996-02-20

Applicant: DEGUSSA

Inventor： KNAUP GUENTER ,  RETZOW STEFAN ,  WECKBECKER CHRISTOPH

IPC: C07D331/04 ,  C07D

CPC classification number: C07D331/04