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    • 11. 发明授权
    • Nucleophile assisting leaving groups
    • 亲核试剂帮助离群
    • US08822707B2
    • 2014-09-02
    • US11667414
    • 2005-11-14
    • Salvatore Lepore
    • Salvatore Lepore
    • C07C309/77C07C309/89C07D323/00C07H11/00
    • C07H11/00C07C309/77C07C309/89C07C2603/74C07D323/00
    • Sulfonate leaving groups include a cation chelating moiety, e.g. a polyether or crown ether. The chelating moiety stabilizes the sulfonate leaving group by forming a complex with a cation of a cation-nucleophile combination. The stabilized leaving group is more easily displaced under many conditions than are standard arylsulfonate leaving groups such as the toxyl group. The chelating moiety also favors certain cations depending on the identity of the moiety thereby enhancing the reaction rate with nucleophilic salts containing the preferred cation. Use of the inventive leaving groups results in improved yields, decreased reaction times and improved product purity.
    • 磺酸盐离去基团包括阳离子螯合部分,例如 聚醚或冠醚。 螯合部分通过与阳离子 - 亲核试剂组合的阳离子形成络合物来稳定磺酸根离去基团。 稳定的离去基团在许多条件下比标准芳基磺酸盐离去基团如甲苯磺酰基更容易置换。 取决于部分的同一性,螯合部分也有利于某些阳离子,从而增强与含有优选阳离子的亲核盐的反应速率。 使用本发明的离去基团导致产率提高,反应时间缩短,产物纯度提高。
    • 12. 发明申请
    • Method for producing substituted phenylsulfonyl urea
    • 取代苯磺酰脲的制备方法
    • US20060004198A1
    • 2006-01-05
    • US10511968
    • 2003-04-16
    • Jan VermehrenMark FordGunter SchlegelIswald OrtBoerries Kuebel
    • Jan VermehrenMark FordGunter SchlegelIswald OrtBoerries Kuebel
    • C07D43/02
    • C07D251/42C07C303/22C07C309/89
    • The invention relates to a preparation process for the compound (I) or a salt thereof where Q, X*, Y, Z, R, R1, R2 and R3 are as defined in claim 1, which comprises a) monoesterifying a compound (II) where Hal=a halogen atom, giving (III), b) either b1) ammonolysing and phosgenating this compound to give (V) or b2) converting this compound with cyanate into (V) and c) converting the resulting compound (V) with the aminoheterocycle H2N-Het (Het=heterocycle as in (I)) into the compound (I) or a salt thereof. Some compounds (II) and some intermediates (VIII), stabilized with N-heteroaromatic compounds, of the compounds (V) are novel. The compounds (II) can be obtained from the corresponding sulfobenzoic acids by reaction with acid halides of sulfur or phosphorus in nonpolar organic solvents.
    • 本发明涉及其中Q,X *,Y,Z,R,R 1,R 2和R 2的化合物(I)或其盐的制备方法 其中包括a)其中Hal =卤素原子的化合物(II)的单酯化,得到(III),b)b1)氨解和光气化该化合物,得到( V)或b2)将该化合物与氰酸酯转化为(V),和c)将所得化合物(V)与氨基杂环H 2 N-Het(Het =如(I)中的杂环))转化成 化合物(I)或其盐。 化合物(V)的一些化合物(II)和一些由N-杂芳族化合物稳定的中间体(VIII))是新颖的。 化合物(II)可以通过在非极性有机溶剂中与硫或磷的酰卤反应从相应的磺基苯甲酸获得。