摘要
L-酪氨酸经三甲基硅烷基保护、磺酰化及脱保护制得N-(丁磺酰基)-L-酪氨酸(5),5与4-(4-氯丁基)吡啶盐酸盐经缩合、钯炭催化加氢及成盐反应制得血小板凝集抑制剂盐酸替罗非班,总收率约60%(以L-酪氨酸计)。
N-（Butylsulfonyl）-L-tyrosine（5） was synthesized from L-tyrosine by silylation with trimethylsilyl chloride,sulfonylation and deprotection.Compound 5 was condensed with 4-（4-chlorobutyl）pyridine hydrochloride,catalytic hydrogenation with Pd/C and salt formation to provide tirofiban hydrochloride.The overall yield was about 60%（based on L-tyrosine）.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2012年第6期408-410,共3页
Chinese Journal of Pharmaceuticals
