Efficient synthesis of 7-amino-3-hydroxyindan-1-one

ORGN 15

Hwa-Ok Kim, kim@creagenbio.com, Raj SB Rajur, Venugopal N. Rao, Pamela Nagafuji, Xavier Hearult, and Norton P. Peet. Department of Chemistry, CreaGen Biosciences, Inc, 23 Rainin Road, Woburn, MA 01801
An efficient and reliable three-step synthesis of 7-amino-3-hydroxyindan-1-one (1) is described. Compound 1 is now an accessible, three-dimensional, three-point scaffold and will be useful for the construction of focused compound libraries. Although indanone 1 has been mentioned in the literature, its preparation has not been recorded and the reported synthesis of its precursor is an experimental procedure that we could not repeat as described. In addition to the synthesis of indanone 1, we describe the preparation of a small set of derivatives that were prepared by functionalization of the amino group, which provides a pilot study for the preparation of a larger library of compounds that will be prepared using semi-automated parallel synthetic methods.