公开(公告)号：US4430510A

公开(公告)日：1984-02-07

申请号：US381250

申请日：1982-05-24

Applicant: Jacques Gosteli

Inventor： Jacques Gosteli

IPC: C07C59/66 ,  B01J23/00 ,  C07B61/00 ,  C07C51/00 ,  C07C51/367 ,  C07C67/00 ,  C07C59/00 ,  C07C65/00

CPC classification number: C07C51/367

Abstract: The present invention relates to a novel process for the preparation of 2-(2,4-dichlorophenoxy)-phenylacetic acid a compound having useful anti-inflammatory properties. The process comprises reacting a 2-halo-phenylacetic acid or a salt thereof under basic conditions in the presence of metallic copper with 2,4-dichlorophenol or a salt thereof.

Abstract translation: 本发明涉及一种制备具有有效抗炎特性的化合物的2-（2,4-二氯苯氧基） - 苯基乙酸的新方法。 该方法包括在碱性条件下在金属铜与2,4-二氯苯酚或其盐的存在下使2-卤代 - 苯乙酸或其盐进行反应。

公开(公告)号：US4320138A

公开(公告)日：1982-03-16

申请号：US214168

申请日：1980-12-08

Applicant: Raymond Bernasconi ,  Pier G. Ferrini ,  Richard Goschke ,  Jacques Gosteli

Inventor： Raymond Bernasconi ,  Pier G. Ferrini ,  Richard Goschke ,  Jacques Gosteli

IPC: A61K31/38 ,  A61K31/381 ,  A61K31/42 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4433 ,  A61P7/02 ,  A61P7/10 ,  A61P19/06 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D333/64 ,  C07D333/68 ,  C07D333/70 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D333/64 ,  C07D333/68 ,  C07D333/70 ,  Y10S514/825

Abstract: Oxothia compounds, especially 2-oxo-2,3-dihydro-benzo[b]-thiophene compounds of the formula ##STR1## in which Ph represents an optionally substituted 1,2-phenylene radical, X represents oxygen or sulphur, R.sub.1 represents an organic radical bonded via a carbon atom and R.sub.2 denotes hydrogen or an optionally substituted hydrocarbon radical of aliphatic character, and their salts are useful as peripheral analgetics and/or as antiphlogistic uricosuric and/or thrombolytic agents.

Abstract translation: 式（Ⅰ）的氧化噻吩化合物，特别是2-氧代-2,3-二氢 - 苯并[b] - 噻吩化合物，其中Ph代表任意取代的1,2-亚苯基，X代表氧或硫， R1表示通过碳原子键合的有机基团，R 2表示氢或任选取代的具有脂族特征的烃基，其盐可用作外周止痛剂和/或作为消炎性尿酸和/或溶栓剂。

公开(公告)号：US4045520A

公开(公告)日：1977-08-30

申请号：US608798

申请日：1975-08-28

Applicant: Jacques Gosteli

Inventor： Jacques Gosteli

IPC: C07F9/38 ,  C07F9/40

CPC classification number: C07F9/4006

Abstract: Thioformamidophosphono-acetates are prepared by reacting an isocyano compound of the formula C=N--CH.sub.2 --X.sub.1 in the presence of a base with a compound of the formula R.sub.o --X.sub.2, in which compounds one of the groups X.sub.1 and X.sub.2 represents a protected carboxyl group of the formula --C(=O)--OR.sub.1 and the other a disubstituted phosphono group of the formula --P(.fwdarw.O)(OR).sub.2, and wherein R.sub.o represents a reactive etherified or esterified hydroxyl group, and adding hydrogen sulphide on to the isocyano group of the phosphono-isocyano-acetate formed as an intermediate.

Abstract translation: 硫代酰氨基膦酰基乙酸酯通过在碱存在下使式C = N-CH 2 -X 1的异氰基化合物与式Ro-X 2化合物反应制备，其中X1和X2基团之一表示保护的羧基 基团-C（= O）-OR1，另一个是式-P（ - ）O（OR）2的二取代膦酰基，其中Ro表示反应性醚化或酯化的羟基，并加入硫化氢 以作为中间体形成的膦酰 - 异氰酸乙酸酯的异氰酸基团。

公开(公告)号：US5484939A

公开(公告)日：1996-01-16

申请号：US208956

申请日：1994-03-11

Applicant: Gareth Griffiths ,  Rene Imwinkelried ,  Jacques Gosteli

Inventor： Gareth Griffiths ,  Rene Imwinkelried ,  Jacques Gosteli

IPC: C07D233/68 ,  C07D233/08

CPC classification number: C07D233/68

Abstract: The 2-substituted 5-chlorimidazoles of general formula: ##STR1## are new intermediate products for the production of antihypertensive pharmaceutical agents or of herbicidal compounds. A process for the production of these intermediate products as well as a new process for the further reaction of 2-substituted 5-chlorimidazoles of general formula I, wherein R.sub.1 is hydrogen, to the 2-substituted 5-chlorimidazole-4-carbaldehydes of general formula: ##STR2##

Abstract translation: 2-取代的5-氯咪唑，其通式如下：图1是生产抗高血压药剂或除草化合物的新中间产物。 制备这些中间体产物的方法以及通式I的其它R 1为氢的2-取代的5-氯咪唑与2-取代的5-取代的5-氯咪唑-4-碳醛进一步反应的新方法 公式： II

公开(公告)号：US5442075A

公开(公告)日：1995-08-15

申请号：US208955

申请日：1994-03-11

Applicant: Gareth Griffiths ,  Rene Imwinkelried ,  Jacques Gosteli

Inventor： Gareth Griffiths ,  Rene Imwinkelried ,  Jacques Gosteli

IPC: C07D233/68 ,  C07D233/70 ,  C07D233/96

CPC classification number: C07D233/68 ,  C07D233/70

Abstract: A process for the production of 2-substituted 5-chlorimidazole-4-carbaldehydes of the general formula: ##STR1## wherein R is hydrogen, an alkyl group, and alkenyl group, a cycloalkyl group, a benzyl group, a phenyl group or an aryl group. These compounds form important intermediate products for the production of antihypertensive pharmaceutical agents or herbicidal compounds.

Abstract translation: 制备以下通式的2-取代的5-氯咪唑-4-碳醛的方法：其中R是氢，烷基和烯基，环烷基，苄基，苯基或 芳基。 这些化合物形成用于生产抗高血压药剂或除草化合物的重要中间产物。

公开(公告)号：US4965359A

公开(公告)日：1990-10-23

申请号：US409743

申请日：1989-09-20

Applicant: Jacques Gosteli ,  Aleksander Warm

Inventor： Jacques Gosteli ,  Aleksander Warm

IPC: C07D211/44 ,  C07D211/74 ,  C07D495/04 ,  C07D513/04

CPC classification number: C07D513/04 ,  C07D211/74

Abstract: A process for the production of 4,5,6,7-tetrahydrothieno-[3,2-c]-pyridines of the formula: ##STR1## Thus, in the case of a 4-oxo-3-piperidine-3-carboxylic acid ester of the formula: ##STR2## an allyl group is introduced in the 3 position, the ester function in the 3 position is removed, the resultant compound of the formula: ##STR3## is ionized, reduced to the corresponding aldehyde of the formula: ##STR4## and with H.sub.2 S/HCl in the presence of a metal halide is cyclized to the end product. The synthesized compounds have antithrombotic action.

Abstract translation: 制备下式的4,5,6,7-四氢噻吩并[3,2-c] - 吡啶的方法：因此，在4-氧代-3-哌啶-3-甲酸 将下式的酸酯引入3位，除去3位的酯官能团，将所得的下式化合物离子化，还原成相应的式 ：在金属卤化物的存在下，使用H 2 S / HCl环化至最终产物。 合成的化合物具有抗血栓作用。

公开(公告)号：US4831084A

公开(公告)日：1989-05-16

申请号：US189294

申请日：1988-05-02

Applicant: Monika Mergler ,  Jacques Gosteli ,  Peter Grogg

Inventor： Monika Mergler ,  Jacques Gosteli ,  Peter Grogg

IPC: C07C43/23 ,  C07C215/78 ,  C07C323/20 ,  C07K1/04 ,  C07K1/113 ,  C07K17/08 ,  C08F8/00 ,  C08F8/26

CPC classification number: C08F8/00 ,  C07K1/042 ,  C08F8/26 ,  C08F8/30 ,  C08F2800/20 ,  Y10S530/815

Abstract: The present invention relates to a novel polymeric carrier, a process for its production and its use for the preparation of peptides and their intermediates. The process comprises reacting chloromethylated polystyrene (cross-linked with divinylbenzene) with a 4-hydroxy-2-substituted-benzyl alcohol (linker), attaching .alpha.-amino acids with amino and side-chain protection to the carrier thus obtained, and building up a peptide according to the method known in the field of solid phase peptide synthesis (SPPS). The method allows removal of intermediates or final products under extremely mild acidic conditions giving products in high state of purity and yield. The 2-substituent consists of an electron donating group, such as methoxy.

Abstract translation: 本发明涉及一种新的聚合物载体，其制备方法及其用于制备肽及其中间体的方法。 该方法包括使氯甲基化聚苯乙烯（与二乙烯基苯交联）与4-羟基-2-取代的苯甲醇（接头）反应，将α-氨基酸与氨基和侧链保护连接到由此获得的载体上，并建立 根据固相肽合成领域已知的方法（SPPS）的肽。 该方法允许在非常温和的酸性条件下除去中间体或最终产物，产生高纯度和高产率的产物。 2-取代基由给电子基团组成，例如甲氧基。

公开(公告)号：US4331676A

公开(公告)日：1982-05-25

申请号：US902639

申请日：1978-05-04

Applicant: Jacques Gosteli ,  Ivan Ernest ,  Robert B. Woodward

Inventor： Jacques Gosteli ,  Ivan Ernest ,  Robert B. Woodward

IPC: C07D499/897 ,  C07D205/08 ,  C07D205/09 ,  C07D499/04 ,  C07D499/06 ,  C07D499/86 ,  C07D499/87 ,  C07D499/88 ,  C07F9/568 ,  C07D499/00

CPC classification number: C07F9/5683 ,  C07D205/09 ,  C07D499/88

Abstract: 2-Penem-3-carboxylic acid compounds of the formula ##STR1## in which R.sub.1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom or an etherified mercapto group andR.sub.2 represents hydroxy or a radical R.sub.2.sup.A forming together with the carbonyl grouping --C(.dbd.O)-- a protected carboxyl group, 1-oxides thereof, as well as salts of such compounds having salt-forming groups, in racemic and optically active form, processes for their preparation, pharmaceutical compositions containing such compounds, and their use as antibiotics, and intermediates and their processes which are useful in the production of the compounds of the formula I.

公开(公告)号：US4260779A

公开(公告)日：1981-04-07

申请号：US92821

申请日：1979-11-09

Applicant: Raymond Bernasconi ,  Pier G. Ferrini ,  Richard Goschke ,  Jacques Gosteli

Inventor： Raymond Bernasconi ,  Pier G. Ferrini ,  Richard Goschke ,  Jacques Gosteli

IPC: C07D333/64 ,  C07D333/68 ,  C07D333/70

CPC classification number: C07D333/68 ,  C07D333/64 ,  C07D333/70 ,  Y10S514/822

Abstract: Oxothia compounds, especially 2-oxo-2,3-dihydro-benzo[b]thiophene compounds of the formula ##STR1## in which Ph represents an optionally substituted 1,2-phenylene radical, X represents oxygen or sulphur, R.sub.1 represents an organic radical bonded via a carbon atom and R.sub.2 denotes hydrogen or an optionally substituted hydrocarbon radical of aliphatic character, and their salts are useful as peripheral analgetics and/or as antiphlogistic uricosuric and/or thrombolytic agents.

Abstract translation: 其中Ph代表任选取代的1,2-亚苯基，X表示氧或硫，R 1，R 2，R 3，R 4，R 4，R 4， 表示通过碳原子键合的有机基团，R 2表示氢或任选取代的脂肪族特征的烃基，其盐可用作外周止痛剂和/或作为消炎性尿酸和/或溶栓剂。

公开(公告)号：US4138451A

公开(公告)日：1979-02-06

申请号：US791757

申请日：1977-04-28

Applicant: Jacques Gosteli

Inventor： Jacques Gosteli

IPC: C07F9/40

CPC classification number: C07F9/4006

Abstract: Thioformamidophosphono-acetates are prepared by reacting an isocyano compound of the formula C.dbd.N--CH.sub.2 --X.sub.1 in the presence of a base with a compound of the formula R.sub.o --X.sub.2, in which compounds one of the groups X.sub.1 and X.sub.2 represents a protected carboxyl group of the formula --C(.dbd.O)--OR.sub.1 and the other a disubstituted phosphono group of the formula --P(.fwdarw.O) (OR).sub.2, and wherein R.sub.o represents a reactive etherified or esterified hydroxyl group, and adding hydrogen sulphide on to the isocyano group of the phosphono-isocyano-acetate formed as an intermediate.

Abstract translation: 硫代酰氨基膦酰基乙酸酯通过在碱存在下使式C = N-CH 2 -X 1的异氰基化合物与式Ro-X 2化合物反应制备，其中X1和X2基团之一表示保护的羧基 基团-C（= O）-OR1，另一个是式-P（ - ）O（OR）2的二取代膦酰基，其中Ro表示反应性醚化或酯化的羟基，并加入硫化氢 以作为中间体形成的膦酰 - 异氰酸乙酸酯的异氰酸基团。