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    • 1. 发明授权
    • Preparation of thiazoles
    • 噻唑的制备
    • US06548676B1
    • 2003-04-15
    • US09331433
    • 1999-06-18
    • Thomas PitternaHenry SzczepanskiPeter MaienfischOttmar Franz HüterThomas RapoldMarcel SennThomas GöbelAnthony Cornelius O'Sullivan
    • Thomas PitternaHenry SzczepanskiPeter MaienfischOttmar Franz HüterThomas RapoldMarcel SennThomas GöbelAnthony Cornelius O'Sullivan
    • C07D27732
    • C07D277/32C07D277/16C07D277/36C07D277/70C07D277/74
    • Described is a process for the preparation of a compound of formula (I) wherein R is unsubstituted or substituted C1-C12alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, aryl or heteroaryl, or —SR1; R1 is unsubstituted or substituted C1-C12alkyl, C2-C4alkenyl, C2-C4alkynyl, cycloalkyl, aryl or heteroaryl; and X is a leaving group; which comprises: a) reacting a compound of formula (II) wherein R is as defined for formula (I), with a water-removing reagent; or b) for the preparation of a compound of formula (I) wherein X is halogen or a sulfonate, reacting a compound of the formula (III) wherein R is as defined for formula (I), with a halogenating or a sulfonylating agent; or c) for the preparation of a compound of formula (I) wherein X is halogen, reacting a compound of formula (IV) wherein R is as defined for formula (I); and wherein R2 and R3 are for example H, C1-C6alkyl, C3-C6cycloalkyl, phenyl or benzyl; with a compound of the formula halogen-C(═O)—O—C1-C8alkyl, halogen-C(═O)—O-aryl or halogen-C(═O)—O-benzyl. Intermediates for the preparation of the synthesis of compounds (II) to (IV) and method of the preparation thereof.
    • 描述了制备式(I)化合物的方法,其中R是未取代的或取代的C 1 -C 12烷基,C 2 -C 4烯基,C 2 -C 4炔基,C 3 -C 6环烷基,芳基或杂芳基或-SR 1; R1是未取代的或取代的C1-C12烷基,C2-C4链烯基,C2-C4炔基,环烷基,芳基或杂芳基; X为离去群; 其包括:a)使其中R如式(I)所定义的式(II)化合物与除水试剂反应; 或者b)用于制备其中X为卤素或磺酸盐的式(I)化合物,其中R为式(I)所定义的式(III)化合物与卤化剂或磺酰化剂反应; 或c)用于制备其中X为卤素的式(I)化合物,其中R为式(I)所定义的式(IV)化合物; 并且其中R 2和R 3是例如H,C 1 -C 6烷基,C 3 -C 6环烷基,苯基或苄基; 与卤素-C(= O)-O-C 1 -C 8烷基,卤素-C(= O)-O-芳基或卤素-C(= O)-O-苄基的化合物反应。 用于制备化合物(II)至(IV)的合成的中间体及其制备方法。