1262506-09-1Relevant articles and documents
An improved process for the preparation of highly pure solifenacin succinate via resolution through diastereomeric crystallisation
Trinadhachari, Ganala Naga,Kamat, Anand Gopalkrishna,Venkata Balaji, Boddu,Prabahar, Koilpillai Joseph,Naidu, Kolukuluru Mohan,Babu, Korupolu Raghu,Sanasi, Paul Douglas
, p. 934 - 940 (2014)
An improved process for the preparation of solifenacin succinate (1) involving resolution through diastereomeric crystallization is described. (1S)-IQL derivative (5) is esterified to form (1S)-ethoxycarbonyl IQL derivative (6) which is condensed with (RS)-3-quinuclidinol (7) to form a solifenacin diastereomeric mixture (8); this is subjected to resolution through diastereomeric crystallization to produce solifenacin succinate (1), which is used for the treatment of an overactive bladder.
A succinic acid thorley that new preparation method
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, (2017/09/19)
The invention relates to a preparation method of succinic acid solifenacin, and belongs to the technical field of medicinal raw material preparation. According to the technical scheme, the preparation method of the novel succinic acid solifenacin is characterized in that R-3-quinuclidinol, S-1-phenyl-1, 2, 3, 4-tetrahydro naphthalene are used as raw materials, a reaction product of triphosgene and substituted phosphine oxide is used as a condensing agent, the solifenacin is prepared through a one-pot method, and then the succinic acid solifenacin is obtained through salifying. The preparation method of the succinic acid solifenacin has the beneficial effects that the operation is simple, reaction conditions are mild, and the preparation method is suitable for industrial amplification production.
After-treatment for solifenacin and method for preparing succinic acid solifenacin
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Paragraph 0062; 0063, (2016/12/01)
The invention discloses an after-treatment method for solifenacin. The method comprises the steps that strong acid is slowly dripped into total synthesis liquid of solifenacin, after a pH value is adjusted to be 1.0-2.0, temperature is raised, water is added, and an extracting agent is used for extraction; after a water phase is cooled, a saturated sodium carbonate solution is added to alkalinity, dichloromethane is added to carry out graded extraction, extract liquor is washed with water, and a drying agent is added for drying, so that a dry product is obtained; the dry product is steamed at low temperature to be dry to obtain an oily substance solifenacin. By optimizing the after-treatment technology, isopropyl ether and dichloromethane are only used in the after-treatment technology of solifenacin, types of solvent are reduced, operation and recycle are facilitated, and cost is saved greatly. Strong base or strong acid is not used in the alkali efflorescence process of hydrochloric acid solifenacin, a saturated NaCO3 solution is used, the reaction is mild, temperature can be controlled easily, most importantly, generation of isomers is greatly reduced, and the content of the isomers of a non-structure type (1S and 3R) is reduced.