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Vol. 29 No. 6 (2017): Vol 29 Issue 6

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Synthesis and Antiviral Activity of Some 1H-Pyrrolo[3,2-b]pyridin-6-yl)acetic Acid Derivatives

https://doi.org/10.14233/ajchem.2017.20372
Hyun-Ah Yoon
Department of Medicinal Chemistry in Korea Research Institute of Science and Technology, 141, Gajung-ro, Yuseong-gu, Daejeon-si, 34114, Republic of Korea
Hwa-Jung Nam
ST PHARM CO., LTD, 231, Hyeomnyeok-ro, Siheung-si, Gyeonggi-do 15086, Republic of Korea
Uk-Il Kim
ST PHARM CO., LTD, 231, Hyeomnyeok-ro, Siheung-si, Gyeonggi-do 15086, Republic of Korea
Kyungjin Kim
ST PHARM CO., LTD, 231, Hyeomnyeok-ro, Siheung-si, Gyeonggi-do 15086, Republic of Korea
Bong Jin Kim
Department of Medicinal Chemistry in Korea Research Institute of Science and Technology, 141, Gajung-ro, Yuseong-gu, Daejeon-si, 34114, Republic of Korea

Corresponding Author(s) : Bong Jin Kim

bjkim@krict.re.kr

Asian Journal of Chemistry, Vol. 29 No. 6 (2017): Vol 29 Issue 6

Abstract

Pyrrolopyridine derivatives for the treatment of HIV1-infection were synthesized by 10 step reactions. Methyl 2-(3-bromo-7-(4-chlorophenyl)-1,5-dimethyl-1H-pyrrolo[3,2-b]pyridin-6-yl)-2-(tert-butoxy) acetate converted efficiently into the corresponding 1H-pyrrolo[3,2-b]pyridin-6-yl)acetic acid derivatives by Suzuki coupling reaction. Present procedure provides short reaction times and good to excellent yields for a wide range of compounds, including pyrrolopyridine scaffolds. 7-Halogenated 1H-pyrrolo[3,2,b]pyridine acetic acid derivatives of final products showed good activity inthe HIV-1 IN inhibition test, while the other derivatives showed relatively low activity.

Keywords

Pyrrolopyridine Suzuki coupling reaction HIV-1 Integrase
Yoon, H.-A., Nam, H.-J., Kim, U.-I., Kim, K., & Kim, B. J. (2017). Synthesis and Antiviral Activity of Some 1H-Pyrrolo[3,2-b]pyridin-6-yl)acetic Acid Derivatives. Asian Journal of Chemistry, 29(6), 1199–1205. https://doi.org/10.14233/ajchem.2017.20372
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