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ChemInform Abstract: An Efficient and Convenient Synthesis of 4,5,6,7-Tetrahydrothieno[3,2-c]pyridines by a Modified Pictet—Spengler Reaction via a Formyliminium Ion Intermediate.

✍ Scribed by Michikazu Kitabatake; Aki Hashimoto; Toshiaki Saitoh; Takehiro Sano; Kunihiko Mohri; Yoshie Horiguchi


Publisher
John Wiley and Sons
Year
2010
Weight
32 KB
Volume
41
Category
Article
ISSN
0931-7597

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✦ Synopsis


Abstract

The Pictet‐Spengler reaction is performed as a one‐pot procedure by condensing thienylethylamine (I) with carbonyl compounds (II), followed by treatment of the in situ formed imines with acetic‐formic anhydride (III) to produce a formyliminium ion, which upon treatment with TFA cyclizes into tetrahydrothienopyridines (IV).