Kilogram synthesis of a LFA-1/ICAM inhibitor

DOI: 10.1021/op9003168

Source and publish data:

Organic Process Research and Development p. 553 - 561 (2010)

Update date:2022-08-05

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Authors:

Delmonte, Albert J.

Waltermire, Robert E.

Fan, Yu Fan, Yu

McLeod, Douglas D.

Gao, Zhinong

Gesenberg, Kirsten D.

Girard, Kevin P.

Rosingana, Miguel

Wang, Xuebao

Kuehne-Willmore, Jennifer

Braem, Alan D.

Castoro, John A.

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Article abstract of DOI:10.1021/op9003168

The process development and the kilogram-scale synthesis of BMS-587101 (1) are described. The synthesis features a [3 + 2] azomethine ylide cycloaddition to efficiently build the spirocyclic core in a diastereoselective fashion followed by a classical res

Full text of DOI:10.1021/op9003168

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