Polymorphic Forms of Dolasetron Base and Processes of Preparing Dolasetron Base, Its Polymorphic Forms and Salt Thereof
申请人:Tarur Venkatasubramanian Radhakrishnan
公开号:US20080275241A1
公开(公告)日:2008-11-06
The present disclosure relates to a process for the preparation of endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-one or Dolasetron base. It also discloses a process for the preparation of endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-one mesylate or Dolasetron mesylate. Further, the present disclosure relates to a process for producing Form I of Dolasetron base, and to the novel crystalline polymorphs, Form II, III, IV and V of Dolasetron base and industrial processes for producing them.
Processes for preparing bicyclo [3.1.0] hexane derivatives, and intermediates thereto
申请人:Hartner W. Frederick
公开号:US20070112030A1
公开(公告)日:2007-05-17
Processes for the preparation of certain [3.1.0]hexane derivatives which are useful as mGluR agonists, and intermediates prepared during such processes.
A 4-acylaminopyrazole derivative represented by the following general formula:
wherein R1 is a hydrogen atom, an optionally substituted C1-C16 alkyl group or the like,
R2 and R3 are independently a hydrogen atom, a halogen atom, an optionally substituted C1-C6 alkyl group or the like,
R4 is a hydrogen atom, a C1-C6 alkyl group or a cyano group,
Z is an oxygen atom or a sulfur atom,
Ar is an optionally substituted C6-C14 aryl group or an optionally substituted 5-6 membered unsaturated heterocyclic group,
B is a hydrogen atom, a halogen atom, an optionally substituted C1-C16 alkyl group or the like.
由以下通式代表的 4-酰氨基吡唑衍生物:
其中 R1 是氢原子、任选取代的 C1-C16 烷基或类似基团、
R2 和 R3 独立地为氢原子、卤素原子、任选取代的 C1-C6 烷基或类似基团、
R4 是氢原子、C1-C6 烷基或氰基、
Z 是氧原子或硫原子、
Ar 是任选取代的 C6-C14 芳基或任选取代的 5-6 位元不饱和杂环基团、
B 是氢原子、卤素原子、任选取代的 C1-C16 烷基或类似基团。