Abrégé

3211 under the condition of a reducing agent; (2) directly adding, without separation, a product obtained from step (1) into alkyne as shown in formula I to perform reaction; and (3) directly adding, without separation, a product obtained from step (2) into an olefin as shown in formula II to perform reaction, thereby obtaining a ruthenium carbene compound as shown in formula III. Gaseous explosive ethylene or acetylene gas is prevented from being applied or generated in a process route; a reaction condition is mild, an extremely low temperature or a high temperature is not required; and an operation is simple. Compared with existing routes, the process has stronger operability and economic advantages.

Classes IPC  ?

• C07F 15/00 - Composés contenant des éléments des groupes 8, 9, 10 ou 18 du tableau périodique
• B01J 31/24 - Phosphines
• B01J 31/22 - Complexes organiques

Abrégé

Disclosed is a highly efficient contrast agent synthesizing method, comprising the following steps: (I) preparing an intermediate mixture of a compound represented by formula (II) and a compound represented by formula (I) and/or formula (III); (II) performing separation to obtain the compound represented by formula (II) and the compound represented by formula (I) and/or formula (III); (III) taking the compound represented by formula (II) to prepare a contrast agent iopromid; and (IV) taking the compound represented by formula (III) to prepare a contrast agent iobitridol; and/or taking a compound represented by formula (I) to prepare a contrast agent iohexol, ioversol, iopentol, or iodixanol. According to the method, by synthesizing and separating intermediates of the compound represented by formula (II) as well as the compound represented by formula (I) and/or formula (III), and then separately preparing contrast agents using the intermediates as the raw materials, the problem of the need to remove a diacylated byproduct in an existing method is overcome, and all intermediates are effectively utilized, the efficiency is high, and the actual application prospect is good.

Classes IPC  ?

• C07C 237/46 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné ayant des atomes de carbone de groupes carboxamide, des groupes amino et au moins trois atomes de brome ou d'iode liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé
• C07C 231/02 - Préparation d'amides d'acides carboxyliques à partir d'acides carboxyliques ou à partir de leurs esters, anhydrides ou halogénures par réaction avec de l'ammoniac ou des amines

Abrégé

Disclosed is a preparation method for a compound shown by formula (E), a Velpatasvir intermediate shown by formula (K) and an analogue thereof. The method of the present invention uses inexpensive and easily available materials, and a simple process operation, without the need for separating the intermediates, the products are by column chromatography, and it is suitable for industrialized large-scale production..

Classes IPC  ?

• C07C 221/00 - Préparation de composés contenant des groupes amino et des atomes d'oxygène, liés par des liaisons doubles, liés au même squelette carboné
• C07C 225/22 - Composés contenant des groupes amino et des atomes d'oxygène, liés par des liaisons doubles, liés au même squelette carboné, au moins un des atomes d'oxygène, liés par des liaisons doubles, ne faisant pas partie d'un groupe —CHO, p. ex. aminocétones ayant des groupes amino liés à des atomes de carbone de cycles aromatiques à six chaînons du squelette carboné
• C07D 311/78 - Systèmes cycliques comportant au moins trois cycles déterminants