发明名称 |
Processes for the preparation of thietanamine |
摘要 |
The present invention provides processes for the preparation of compounds of formula (I) including processes comprising a. reacting a compound of formula (II) with a nucleophile in the presence of water to give a compound comprising a thietane moiety in which the carbon atom at the 3 position of the thietane moiety is bonded to a nitrogen atom; wherein the nucleophile is selected the group consisting of: N3−, a sulfonamide having two hydrogen atoms bound to the nitrogen atom, a diimide having a hydrogen atom bound to the nitrogen atom or an anion thereof, NH2OH and NH3; and b. when the nucleophile used in step a. is N3− or NH2OH, reacting the compound produced in step a. with a suitable reducing agent to give a compound of formula (I); or when the nucleophile used in step a. is a sulfonamide, reacting the compound produced in step a. with a reagent suitable for cleaving the S—N bond of the sulfonamide group to give a compound of formula (I); or when the nucleophile used in step a. is a diimide, reacting the compound produced in step a. with a reagent suitable for cleaving the C—N bond of the amide group to give a compound of formula (I). The invention also relates to intermediates useful for the preparation of compounds of formula (I).; |
申请公布号 |
US9006456(B2) |
申请公布日期 |
2015.04.14 |
申请号 |
US201214131284 |
申请日期 |
2012.07.05 |
申请人 |
Syngenta Participations AG |
发明人 |
Cassayre Jerome Yves;Godineau Edouard;Boussemghoune Mohamed Abdelouahab;Smits Helmars |
分类号 |
C07D331/04;C07D409/12;C07D409/04 |
主分类号 |
C07D331/04 |
代理机构 |
|
代理人 |
Jones R. Kody |
主权项 |
1. A process for the preparation of a compound of formula I comprising a. reacting a compound of formula II with a nucleophile in the presence of water to give a compound comprising a thietane moiety in which the carbon atom at the 3 position of the thietane moiety is bonded to a nitrogen atom; wherein the nucleophile is selected the group consisting of: N3−, a sulfonamide having two hydrogen atoms bound to the nitrogen atom, a diimide having a hydrogen atom bound to the nitrogen atom or an anion thereof, NH2OH and NH3; and b. when the nucleophile used in step a. is N3− or NH2OH, reacting the compound produced in step a. with a suitable reducing agent to give a compound of formula I; or when the nucleophile used in step a. is a sulfonamide, reacting the compound produced in step a. with a reagent suitable for cleaving the S—N bond of the sulfonamide group to give a compound of formula I; or when the nucleophile used in step a. is a diimide, reacting the compound produced in step a. with a reagent suitable for cleaving the C—N bond of the amide group to give a compound of formula I. |
地址 |
Basel CH |