Transition-metal-catalyzed chlorosulfonylation of 5-ethynylpyrimidine nucleosides provided (E)-5-(β-chlorovinyl)sulfones A, which undergo nucleophilic substitution with amines or thiols affording B. The treatment of vinyl sulfones A with ammonia followed by acid-catalyzed hydrolysis of the intermediary β-sulfonylvinylamines gave 5-(β-keto)sulfones C. The latter reacts with electrophiles, yielding α-carbon-alkylated or -sulfanylated analogues D. The 5′-triphosphates of A and C were incorporated into double-stranded DNA, using open and one-nucleotide gap substrates, by human or Escherichia coli DNA-polymerase-catalyzed reactions.

中文翻译：

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在C5位具有反应性（β-氯丁酰基）砜或（β-酮）砜基的嘧啶核苷，它们与亲核试剂和亲电试剂的反应以及它们聚合酶催化的掺入DNA

的提供（5- ethynylpyrimidine核苷过渡金属催化的氯磺酰化ë）-5-（β氯乙烯基）砜甲，其经历与胺或硫醇，得到亲核取代乙。乙烯基的治疗砜阿与氨，接着由中间β-sulfonylvinylamines的酸催化的水解，得到5-（β -酮）砜Ç。后者发生反应与亲电子，得到α -碳-烷基化或-sulfanylated类似物d。A和C的5'-三磷酸通过人或大肠杆菌通过开放和一个核苷酸的缺口底物掺入双链DNA中 DNA聚合酶催化的反应。