The present invention provides processes for the preparation of compounds of formula (I) including processes comprising a. reacting a 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: N
3
−
, 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, NH
2
OH and NH
3
; and b. when the nucleophile used in step a. is N
3
−
or NH
2
OH, 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).
本发明提供了制备式(I)化合物的方法,包括以下步骤:a.反应含有
噻吩环的化合物,其中
噻吩环的3位碳原子与氮原子键合;其中亲核试剂选择如下组:N3−,一个含有两个氢原子与氮原子键合的磺酰胺,一个含有氢原子与氮原子键合或其阴离子的二亚甲基,NH2OH和NH3; b.当步骤a中使用的亲核试剂为N3−或NH2OH时,用适当的还原剂反应步骤a中产生的化合物,以得到式(I)化合物;或者当步骤a中使用的亲核试剂为磺酰胺时,用适合裂解磺酰胺基团的试剂反应步骤a中产生的化合物,以得到式(I)化合物;或者当步骤a中使用的亲核试剂为二亚甲基时,用适合裂解酰胺基团的试剂反应步骤a中产生的化合物,以得到式(I)化合物。本发明还涉及用于制备式(I)化合物的中间体。