Synthesis of a new class of cathepsin B inhibitors exploiting a unique reaction cascade
โ Scribed by Yoshimitsu Nagao; Shigeki Sano; Kenji Morimoto; Hisao Kakegawa; Tadanobu Takatani; Motoo Shiro; Nobuhiko Katunuma
- Publisher
- Elsevier Science
- Year
- 2000
- Tongue
- French
- Weight
- 223 KB
- Volume
- 41
- Category
- Article
- ISSN
- 0040-4039
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โฆ Synopsis
Chiral 5-substituted 3-pyrrolin-2-ones bearing L-Ile-L-Pro-OH or L-Phe-NHCH 2 Ph were successfully synthesized by utilizing a characteristic reaction cascade based on alkaline hydrolysis of the corresponding diethyl ฮฑhydroxy-ฮฑ-(ฮฒ-propiolamide)malonates. Among the synthesized chiral pyrrolinones, compound 5S-9 proved to be the most potent inhibitor against cathepsin B.
๐ SIMILAR VOLUMES
## Abstract magnified image A novel cascade reaction of 4โarylideneโ2โphenylโ1,3โoxazolโ5(4__H__)โone with 3โmethylโ1โphenylโ1__H__โpyrazolโ5โamine was described and a number of new pyrazolo[3,4โ__b__]pyridineโ6โone derivatives were synthesized. This new protocol has the advantages of shorter time
Scheme 1. Retrosynthetic analysis of the cycloocta[b]indole target structure.