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Kaoru Fuji's Special Issues, Vol. 101, No. 2, 2020

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Short Paper | Special issue | Vol 101, No. 2, 2020, pp. 717 - 725
Published online: 10th October, 2019
DOI: 10.3987/COM-19-S(F)50
Lewis Acid Mediated Synthesis of Indolizidine Derivatives

Sambasivarao Kotha* and Sunil Pulletikurti

*Department of Chemistry, Indian Institute of Technology Bombay, Powai, Mumbai - 400076, India

Abstract

Here, we have reported a short and efficient BF3Et2O catalyzed synthesis of indolizidine derivatives. Morever, we have expanded this strategy to synthesize oxa-aza-cyclic derivatives. The stereochemistry of the indolizidine derivative 16 was confirmed by X-ray studies.

Supporting Info. (2.2MB)PDF (1MB)PDF with Links (852KB)
Short Paper | Special issue | Vol 101, No. 2, 2020, pp. 726 - 737
Published online: 23rd October, 2019
DOI: 10.3987/COM-19-S(F)52
Design, Synthesis and Structure-Activity Relationship Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors

Seiya Hiranaka, Mayumi Arata, Akiko Nakata, Akiko Tanaka, Yoshinobu Hashizume, Norio Kudo, Akihiro Ito, Minoru Yoshida, Shinichi Uesato, Yasuo Nagaoka, and Takaaki Sumiyoshi*

*Faculty of Chemistry, Materials and Bioengineering, Kansai University, 3-3-35 Yamate-cho, Suita, Osaka 564-8680, Japan

Abstract

For the study on the structure-activity relationship of pyrilamine-based histone deacetylase inhibitor 1, we focused on the structures of its benzyl and dimethylamino groups. Of the synthesized novel pyrilamine derivatives 27, compound 2 enhanced potency against hERG inhibition, as well as decreased molecular weight and topological polar surface area.

Supporting Info. (809KB)PDF (1.2MB)PDF with Links (762KB)
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