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    • 8. 发明申请
    • PHOTOLYTICALLY CLEAVABLE ENCODING AND LINKING AGENTS FOR USE IN COMBINATORIAL CHEMISTRY
    • 用于组合化学的光致可清除编码和连接试剂
    • WO1996030337A1
    • 1996-10-03
    • PCT/US1996004414
    • 1996-03-29
    • SMITHKLINE BEECHAM CORPORATIONGARIGIPATI, Ravi, ShankerADAMS, Jerry, Leroy
    • SMITHKLINE BEECHAM CORPORATION
    • C07C311/16
    • C07C311/16B01J2219/00572C40B70/00
    • The present invention is to novel photochemically cleavable aryl sulfonamides of the formula: P-A3-A2-A1-S(O)2NR1R2 wherein: R1 and R2 are independently selected from optionally substituted alkyl, arylalkyl or heteroarylalkyl; A1 is an aryl or heteroaryl moiety; A2 is a linking agent is an aryl, heteroaryl, arylalkyl, heteroaryl alkyl, or an alkyl, wherein the alkyl moiety in the arylalkyl, heteroaryl alkyl, or alkyl group is optionally interrupted one or more times independently by oxygen, NR3, sulfur or an amide group; R3 is alkyl; A3 is an electron rich aryl or heteroaryl moiety having an E1/2 potential of 0.5 to 2.0 and which moiety is capable of forming an exciplex; P is a solid support. Another aspect of the present invention is to the novel use of these photolytically cleavable aryl sulfonamides in combinatorial chemistry synthesis, for use in non-sequential encoding, as a tagging agent. Another aspect of the present inevention is to the novel use of these photolytically cleavable aryl sulfonamides in combinatorial chemistry synthesis, as a linking agent which is bound to a solid support, and upon photolytic cleavage will provide a free amine of the desired final products, i.e. the use of sulfonamides for the solid phase synthesis of amines.
    • 本发明是新型的具有下式的光化学可裂解的芳基磺酰胺:P-A3-A2-A1-S(O)2NR1R2其中:R1和R2独立地选自任选取代的烷基,芳基烷基或杂芳基烷基; A1是芳基或杂芳基部分; A2是连接剂是芳基,杂芳基,芳基烷基,杂芳基烷基或烷基,其中芳基烷基,杂芳基烷基或烷基中的烷基部分任选地被氧,NR 3,硫或 酰胺基; R3是烷基; A3是具有0.5至2.0的E1 / 2电位的电子富集的芳基或杂芳基部分,并且该部分能够形成激元复合体; P是一个坚实的支持。 本发明的另一方面是这些光可裂解的芳基磺酰胺在组合化学合成中的新用途,用于非顺序编码作为标记试剂。 本发明的另一个方面是这些光可裂解的芳基磺酰胺在组合化学合成中的新用途,作为与固体支持物结合的连接剂,并且在光解裂解时将提供所需最终产物的游离胺,即 使用磺酰胺进行固相合成胺。