中国医药工业杂志
中國醫藥工業雜誌
중국의약공업잡지
CHINESE JOURNAL OF PHARMACEUTICALS
2009年
8期
561-562
,共2页
邹霈%罗世能%谢敏浩%刘娅灵%何拥军
鄒霈%囉世能%謝敏浩%劉婭靈%何擁軍
추패%라세능%사민호%류아령%하옹군
碘他拉酸%离子型X线造影剂%合成
碘他拉痠%離子型X線造影劑%閤成
전타랍산%리자형X선조영제%합성
iothalamic acid%ionic X-ray contrast agent%synthesis
5-硝基-1,3-苯二甲酸单甲酯和40%甲胺水溶液经酰胺化反应得到3-硝基-5-[(甲胺基)羰基]苯甲酸,再经Pd/C催化氢化还原和氯化碘碘代得到3-氨基-2,4,6.三碘-5-[(甲胺基)羰基]苯甲酸,最后经乙酰化反应制得离子型x线造影剂碘他拉酸,总收率约80%.
5-硝基-1,3-苯二甲痠單甲酯和40%甲胺水溶液經酰胺化反應得到3-硝基-5-[(甲胺基)羰基]苯甲痠,再經Pd/C催化氫化還原和氯化碘碘代得到3-氨基-2,4,6.三碘-5-[(甲胺基)羰基]苯甲痠,最後經乙酰化反應製得離子型x線造影劑碘他拉痠,總收率約80%.
5-초기-1,3-분이갑산단갑지화40%갑알수용액경선알화반응득도3-초기-5-[(갑알기)탄기]분갑산,재경Pd/C최화경화환원화록화전전대득도3-안기-2,4,6.삼전-5-[(갑알기)탄기]분갑산,최후경을선화반응제득리자형x선조영제전타랍산,총수솔약80%.
Iothalamic acid, an ionic X-ray contrast agent was synthesized from monomethyl 5-nitroisophthlate and methylamine by amidation to give 3-nitro-5- [(methylamino) carbonyl]benzoic acid, which was subjected to catalytic hydrogenation and iodination to afford 3-amino-2,4,6-triiodo-5-[(methylamino)carbonyl]benzoic acid, followed by acetylation with acetic anhydride with an overall yield of about 80 %.