公开(公告)号：US4761495A

公开(公告)日：1988-08-02

申请号：US690682

申请日：1985-01-11

申请人： Didier Wirth ,  Dominique Gibert ,  Annie Boutin

发明人： Didier Wirth ,  Dominique Gibert ,  Annie Boutin

IPC分类号： C07K1/00 ,  C07K5/075 ,  C07K14/575 ,  C07C101/02 ,  C07C69/00 ,  C07C101/24 ,  C07C101/26

CPC分类号： C07K5/0613 ,  Y02P20/55

摘要： The present invention is directed to a composition and method relating to the preparation of aspartyl peptides having the general formula: ##STR1## where the radical-NHR represents an amino acid or peptide group. In the method, a .beta.-monoester of aspartic acid having the general formula: ##STR2## where R.sub.1 represents a hydrocarbon-containing radical, is reacted with a .beta.-dicarbonyl compound, preferably ethylacetoacetate to protect the aspartyl amino group and form an enamine. The enamine is then coupld to an amino acid or peptide, following which any protecting groups are removed to yield .alpha.-aspartyl peptides without any .beta.-isomer. In its composition aspects, the present invention is directed to novel enamines resulting from reaction of the .beta.-monoester of aspartic acid with a .beta.-dicarbonyl compound.

摘要翻译： 本发明涉及与制备具有以下通式的天冬氨酰肽有关的组合物和方法：其中自由基-NHR代表氨基酸或肽基团。 在该方法中，具有以下通式的天冬氨酸的β-单酯：其中R 1表示含烃基团的天冬氨酸与β-二羰基化合物，优选乙酰乙酰乙酸酯反应以保护天冬氨酰氨基并形成烯胺。 然后将烯胺偶联成氨基酸或肽，随后除去任何保护基团以产生没有任何β-异构体的α-天冬酰胺肽。 在其组成方面，本发明涉及由天冬氨酸的β-单酯与β-二羰基化合物反应得到的新型烯胺。

公开(公告)号：US3987042A

公开(公告)日：1976-10-19

申请号：US621617

申请日：1975-10-10

申请人： Claude Gueremy ,  Robert Labey ,  Didier Wirth ,  Maurice Auclair

发明人： Claude Gueremy ,  Robert Labey ,  Didier Wirth ,  Maurice Auclair

IPC分类号： C07D453/02

CPC分类号： C07D453/02

摘要： Phenothiazine derivatives are described of the formula ##SPC1##In which X.sub.1 and X.sub.2, which may be the same or different, are H, R, F, Cl, Br, OR, CN, --COR, CH.sub.3, --S--R, --SOR, --SO.sub.2 R or --SO.sub.2 N(CH.sub.3).sub.2, where R is an alkyl group having from 1 to 4 carbon atoms, and the quinuclidine ring is substituted by the group --(CH.sub.2).sub.x -- in the 2- or 3- position, x being 1 or 2 when said group is substituted in the 2-position and being 0 or 1 when said group is substituted in the 3-position (because of electronic hindrance), and their acid addition and quaternary ammonium salts, have valuable pharmacological properties. In particular, these compounds have anti-histaminic, anti-cholinergic, adrenolytic, neuro-sedative, tranquillizing and/or spasmolytic properties.These compounds are prepared by condensing an appropriate phenothiazine with a quinuclidine derivative of the formula ##SPC2##In which x has the above-stated meaning and Z is a halogen atom or a reactive ester group.