摘要:
The present invention relates to a process for the preparation of a 4,5-diamino shikimic acid derivative of formula (I) and pharmaceutically acceptable addition salts thereof wherein R 1 , R 1’ are independent of each other H or alkyl, R 2 is an alkyl and R 3 , R 4 are independent of each other H or an alkanoyl, with the proviso that not to both R 3 and R 4 are H. 4,5-diamino shikimic acid derivatives of formula I, especially the (3R,4R,5S)-5-amino-4-acetylamino-3- (1-ethyl-propoxy)-cyclohex-l-ene-carboxylic acid ethyl ester and its pharmaceutically acceptable additional salts are potent inhibitors of viral neuraminidase.
摘要:
The invention concerns compounds of formula (1) wherein in particular G represents the -N(CH3)2-, -N(C2H5)2-group or N-pyrrolidine; n is an integer equal to 1 or 2; R1, R2 and R3, independently of one another, represent a hydrogen atom or a methyl group, the successive unsaturated units capable of being moreover identical or different, provided that at least one of the substituents R1, R2 and R3 is different from H; and Y1 and Y2 represent each a -COOCH3 group or a -COOC2H5 group.
摘要翻译:本发明涉及式(1)的化合物,其中特别地,G表示-N(CH 3)2 - , - N(C 2 H 5)2 - 基或N-吡咯烷; n是等于1或2的整数; R1,R2和R3彼此独立地表示氢原子或甲基,连续的不饱和单元能够进一步相同或不同,条件是取代基R 1,R 2和R 3中的至少一个不同于H; Y 1和Y 2分别表示-COOCH 3基或-COOC 2 H 5基。
摘要:
A process for making alkyl 6-aminocaproate by hydroformylating 3-pentenenitrile to produce 3-, 4-, and 5-formylvaleronitrile (FVN mixture), converting the FVN mixture to alkyl 3-, 4-, and 5-cyanovalerate by either oxidative esterification of the FVN mixture or oxidation of the FVN mixture followed by esterification; isolating alkyl 5-cyanovalerate; and hydrogenating the alkyl 5-cyanovalerate to produce alkyl 6-aminocaproate. The resulting alkyl 6-aminocaproate can be cyclized to produce caprolactam.
摘要:
The invention concerns compounds of formula (1) wherein in particular G represents the -N(CH3)2-, -N(C2H5)2-group or N-pyrrolidine; n is an integer equal to 1 or 2; R1, R2 and R3, independently of one another, represent a hydrogen atom or a methyl group, the successive unsaturated units capable of being moreover identical or different, provided that at least one of the substituents R1, R2 and R3 is different from H; and Y1 and Y2 represent each a -COOCH3 group or a -COOC2H5 group.
摘要:
The invention concerns benzodiazepinone derivatives of formula (I) wherein: R1, R2 [A1] and [A2] are as defined in the description, their preparation method and intermediates therefor, their use as medicines, in particular as anti-absorption agent and pharmaceutical compositions containing them.
摘要:
An imine fixed to a resin characterized in that it is represented by the following formula: P-Q-N=CH-R wherein P represents a main chain of a polymer constituting the resin, Q represents a hydrocarbon side chain optionally substituted with a substituent which may be bonded via a heteroatom and R represents an optionally substituted hydrocarbon group or a heterocyclic group, and a beta -aminocarbonyl compound fixed to a resin represented by formula (II) are provided. The beta -aminocarbonyl compound fixed to a resin is a beta -aminocarbonyl compound being handled in a solid form. An amine fixed to a resin which is a key compound for a solid state synthesis of this type and represented by the following formula: P-Q1-O-Q2-NH2, wherein Q1 and Q2 are each a hydrocarbon chain selected from among an arylene group, an alkylarylene group and an arylenealkylene group, is also provided, which allows the synthesis of beta -aminocarbonyl compound by application of an iminoaldol reaction in a solid phase.
摘要:
L'invention concerne un procédé de préparation d'un dérivé d'acide 11 -aminoundécanoïque ou 12-aminododécanoïque, ou d'un ester de celui-ci, de formule R-NH-(CH 2 ) n -COOR', dans laquelle n vaut 10 ou 11, R représente un groupement alkyle, fluoroalkyle, benzyle ou alkylbenzyle, et R' représente un atome d'hydrogène ou un groupement alkyle, le procédé comprenant : la réaction du composé de départ de formule NH 2 -(CH 2 ) n -COOR' avec l'aldéhyde de formule R=O dans un solvant halogéné, pour former un composé imine de formule R=N-(CH 2 ) n -COOR'; et - la réduction du composé imine.
摘要:
This invention relates to methods for making oxetan-3-ylmethanamines having the formula (I) wherein R1? and R2? are as defined herein. The methods of the invention provide the compounds of formula (I) in high yields and under conditions amenable for large-scale commercial production.