Diastereoselective synthesis of spiro-[cyclopropane-1,3 '-indolin]-2 '-ones through metal-free cyclopropanation using tosylhydrazone salts

作者：Kapure Jeevak Sopanrao; Reddy Chada Narsimha; Adiyala Praveen Reddy; Nayak Ranjita; Nayak V Lakshma; Nanubolu Jagadeesh Babu; Singarapu Kiran Kumar; Maurya Ram Awatar^*

来源：RSC Advances, 2014, 4(72): 38425-38432.

DOI：10.1039/c4ra05755d

Transition metal-free diastereoselective cyclopropanation of 3-methyleneindolin-2-ones using tosylhydrazone salts as a safe alternative to diazo-compounds was achieved in high yields. All the synthesized compounds were evaluated for their biological activity against three different human cancer cell lines DU-145 (prostate cancer), Hela (cervical cancer) and A-549 (lung cancer). Compounds 3b and 3i exhibited promising anticancer activity (IC50 < 10 mu M) against the studied cell lines.

• 出版日期2014