Dehydrogenative [2 + 2 + 1] Heteroannulation Using a Methyl Group as a One-Carbon Unit: Access to Pyrazolo[3,4-c]quinolines

Dehydrogenative [2 + 2 + 1] Heteroannulation Using a Methyl Group as a One-Carbon Unit: Access to Pyrazolo[3,4-c]quinolines

Guo-Bo Deng^†, Hai-Bing Li^†, Xu-Heng Yang^†, Ren-Jie Song^*†, Ming Hu^†, and Jin-Heng Li^*†‡

^† State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China

^‡ State Key Laboratory of Applied Organic Chemistry Lanzhou University, Lanzhou 730000, China

Org. Lett., Article ASAP

DOI: 10.1021/acs.orglett.6b00618

Publication Date (Web): April 28, 2016

Copyright © 2016 American Chemical Society

*E-mail: srj0731@hnu.edu.cn., *E-mail: jhli@hnu.edu.cn.

http://pubs.acs.org/doi/abs/10.1021/acs.orglett.6b00618

 A practical and straightforward access to pyrazolo[3,4-c]quinolines by molecular sieve mediated dehydrogenative [2 + 2 + 1] heteroannulation of N-(o-alkenylaryl)imines with aryldiazonium salts is described using a sp³-hybrid carbon atom as a one-carbon unit. The reaction enables the formation of three new chemical bonds, a C–C bond and two C–N bonds, in a single reaction and features simple operation and excellent functional group tolerance.

/////////Dehydrogenative [2 + 2 + 1] Heteroannulation,   Pyrazolo[3,4-c]quinolines

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Inductive electrospray ionization (iESI) is an ambient ionization method that is particularly well-suited to online reaction monitoring. It allows the potential of electrospray mass spectrometry (MS) to be realized as a routine process analytical technology (PAT) tool to monitor practical synthetic reactions in real time. In this study, a synthetic route to Anagliptin (target API) was successfully monitored using online iESI-MS. Starting materials not seen by traditional reaction monitoring tools (HPLC-UV/Vis and GC-FID) were observed, as well as water-sensitive reagents and intermediates which cannot easily be followed by other methods. Online tandem mass spectrometry (MS/MS) was used to characterize chemical species in the reaction mixture. Impurities and byproducts were identified, and information on the progress of byproduct formation enabled implementation of strategies to eliminate these byproducts in the course of the reaction. This work demonstrates how iESI-MS can be employed to obtain comprehensive information and solutions to some practical problems that occur in small-molecule synthetic reaction monitoring.

Online Inductive Electrospray Ionization Mass Spectrometry as a Process Analytical Technology Tool To Monitor the Synthetic Route to Anagliptin

Xin Yan†, Ryan M. Bain†, Yafeng Li†, Ran Qiu†, Tawnya G. Flick*‡, and R. Graham Cooks*†

† Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, United States

‡ Department of Analytical Research & Development, Amgen Inc., 1 Amgen Center Drive, Thousand Oaks, California 91320, United States

Org. Process Res. Dev., Article ASAP

DOI: 10.1021/acs.oprd.6b00039

Publication Date (Web): April 12, 2016

Copyright © 2016 American Chemical Society

*E-mail for T.G.F.: tflick@amgen.com., *E-mail for R.G.C.: cooks@purdue.edu.

http://pubs.acs.org/doi/abs/10.1021/acs.oprd.6b00039

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