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    • 3. 发明授权
    • Processes for the preparation of thietanamine
    • 制备泰安胺的方法
    • US09006456B2
    • 2015-04-14
    • US14131284
    • 2012-07-05
    • Jerome Yves CassayreEdouard GodineauMohamed Abdelouahab BoussemghouneHelmars Smits
    • Jerome Yves CassayreEdouard GodineauMohamed Abdelouahab BoussemghouneHelmars Smits
    • C07D331/04C07D409/12C07D409/04
    • C07D331/04C07D409/04C07D409/12
    • 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).
    • 本发明提供制备式(I)化合物的方法,包括以下步骤:a。 在水存在下使式(II)化合物与亲核试剂反应,得到包含硫杂环丁烷部分的化合物,其中硫杂环丁烷部分的3位的碳原子与氮原子结合; 其中所述亲核试剂选自:N 3 - ,具有与氮原子结合的2个氢原子的磺酰胺,具有与氮原子结合的氢原子的二酰亚胺或其阴离子,NH 2 OH和NH 3; 和b。 当步骤a中使用亲核试剂时。 是N 3 - 或NH 2 OH,使步骤a中制备的化合物。 与合适的还原剂反应,得到式(I)化合物; 或当步骤a中使用的亲核试剂时。 是磺酰胺,使步骤a中制备的化合物反应。 用适于切割磺酰胺基团的S-N键的试剂得到式(I)化合物; 或当步骤a中使用的亲核试剂时。 是二酰亚胺,使步骤a中制备的化合物反应。 用适于切割酰胺基团的C-N键的试剂得到式(I)的化合物。 本发明还涉及可用于制备式(I)化合物的中间体。
    • 4. 发明申请
    • PROCESSES FOR THE PREPARATION OF THIETANAMINE
    • 制备噻吩胺的方法
    • US20140187788A1
    • 2014-07-03
    • US14131284
    • 2012-07-05
    • Jerome Yves CassayreEdouard GodineauMohamed Abdelouahab BoussemghouneHelmars Smits
    • Jerome Yves CassayreEdouard GodineauMohamed Abdelouahab BoussemghouneHelmars Smits
    • C07D331/04C07D409/04
    • C07D331/04C07D409/04C07D409/12
    • 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: 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).
    • 本发明提供制备式(I)化合物的方法,包括以下步骤:a。 使含有硫杂环丁烷部分的化合物与硫原子部分3位的碳原子键合在氮原子上; 其中所述亲核试剂选自:N 3 - ,具有与氮原子结合的2个氢原子的磺酰胺,具有与氮原子结合的氢原子的二酰亚胺或其阴离子,NH 2 OH和NH 3; 和b。 当步骤a中使用亲核试剂时。 是N 3 - 或NH 2 OH,使步骤a中制备的化合物。 与合适的还原剂反应,得到式(I)化合物; 或当步骤a中使用的亲核试剂时。 是磺酰胺,使步骤a中制备的化合物反应。 用适于切割磺酰胺基团的S-N键的试剂得到式(I)化合物; 或当步骤a中使用的亲核试剂时。 是二酰亚胺,使步骤a中制备的化合物反应。 用适于切割酰胺基团的C-N键的试剂得到式(I)的化合物。 本发明还涉及可用于制备式(I)化合物的中间体。