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Microwave Heated Fl...
Microwave Heated Flow Synthesis of Spiro-oxindole Dihydroquinazolinone Based IRAP Inhibitors
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- Engen, Karin (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Sävmarker, Jonas (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Rosenström, Ulrika (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi,Plattformen för preklinisk PET
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- Wannberg, Johan (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Lundbäck, Thomas (author)
- Karolinska Institutet
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- Jenmalm-Jensen, Annika (author)
- Karolinska Institutet
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- Larhed, Mats (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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(creator_code:org_t)
- 2014-10-16
- 2014
- English.
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In: Organic Process Research & Development. - : American Chemical Society (ACS). - 1083-6160 .- 1520-586X. ; 18:11, s. 1582-1588
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http://pubs.acs.org/...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- A fast and convenient synthetic route towards spiro-oxindole dihydroquinazolinones as novel and drug-like insulin-regulated aminopeptidase (IRAP) inhibitors is reported. The synthesis is performed using a MW heated continuous flow system employing 200 mm X 3 mm i MW absorbing silicon carbide (SiC) or MW transparent borosilicate tubular reactors. A three-component MW-flow reaction to build up the spiro compounds (9 examples, 4087% yield), using the SiC reactor, as well as a SuzukiMiyaura cross-coupling reaction (71%), employing the borosilicate reactor, are presented with residence times down to 168 s. The continuous MW-flow routes provide a smooth and scalable synthetic methodology towards this class of IRAP inhibitors.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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