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The Development of a Large-Scale Synthesis of Matrix Metalloproteinase Inhibitor, ABT-518
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2002-05-01 , DOI: 10.1021/op025525l Sou-Jen Chang 1 , Dilinie Fernando 1 , Michael Fickes 1 , Ashok K. Gupta 1 , David R. Hill 1 , Todd McDermott 1 , Shyamal Parekh 1 , Zhenping Tian 1 , Steven J. Wittenberger 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2002-05-01 , DOI: 10.1021/op025525l Sou-Jen Chang 1 , Dilinie Fernando 1 , Michael Fickes 1 , Ashok K. Gupta 1 , David R. Hill 1 , Todd McDermott 1 , Shyamal Parekh 1 , Zhenping Tian 1 , Steven J. Wittenberger 1
Affiliation
A process for the preparation of matrix metalloproteinase inhibitor ABT-518 has been developed. Significant improvements have been made to the first generation synthesis and are described here. The new process is very robust and efficient; multikilogram quantities of the title compound have been synthesized for clinical trials. ABT-518 was prepared by this six-step synthetic sequence in 51% overall yield with >99% ee.
中文翻译:
大规模合成基质金属蛋白酶抑制剂 ABT-518
已经开发了一种制备基质金属蛋白酶抑制剂 ABT-518 的方法。对第一代合成进行了重大改进,并在此处进行了描述。新流程非常稳健和高效;已合成数公斤量的标题化合物用于临床试验。ABT-518 通过这个六步合成序列以 51% 的总产率和 >99% 的 ee 制备。
更新日期:2002-05-01
中文翻译:
大规模合成基质金属蛋白酶抑制剂 ABT-518
已经开发了一种制备基质金属蛋白酶抑制剂 ABT-518 的方法。对第一代合成进行了重大改进,并在此处进行了描述。新流程非常稳健和高效;已合成数公斤量的标题化合物用于临床试验。ABT-518 通过这个六步合成序列以 51% 的总产率和 >99% 的 ee 制备。