152714-07-3Relevant articles and documents
A simple and efficient new approach to the total synthesis of (±)-4- amino-3-(4-chlorophenyl)-butyric acid (BACLOFEN)
Coelho, Fernando,De Azevedo, Mariangela B. M.,Boschiero, Roberta,Resende, Patricia
, p. 2455 - 2465 (1997)
Based on the utilization of a [2+21 cycloaddition reaction between dichloroketene and an appropriated olefin as a key step, we describe a new and simple four step approach to the total synthesis of (±)-4-amino-3-(4- chlorophenyl)-butyric acid (BACLOFEN),
Desymmetrization of Prochiral Cyclobutanones via Nitrogen Insertion: A Concise Route to Chiral γ-Lactams
Sietmann, Jan,Ong, Mike,Mück-Lichtenfeld, Christian,Daniliuc, Constantin G.,Wiest, Johannes M.
supporting information, p. 9719 - 9723 (2021/03/16)
Asymmetric access to γ-lactams is achieved via a cyclobutanone ring expansion using widely available (1S,2R)-1-amino-2-indanol for chiral induction. Mechanistic analysis of the key N,O-ketal rearrangement reveals a Curtin–Hammett scenario, which enables a downstream stereoinduction (up to 88:12 dr) and is corroborated by spectroscopic, crystallographic, and computational studies. In combination with an easy deprotection protocol, this operationally simple sequence allows the synthesis of a range of optically pure γ-lactams, including those bearing all-carbon quaternary stereocenters. In addition, the formal synthesis of drug molecules baclofen, brivaracetam, and pregabalin further demonstrates the synthetic utility and highlights the general applicability of the presented method.
CARBOXAMIDE AND SULFONAMIDE DERIVATIVES USEFUL AS TEAD MODULATORS
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Paragraph 0413-0417, (2020/03/29)
The invention is concerned with the compounds of formula (I) and formula (II): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of using the compounds of formula (I) and formula (II) as well as pharmaceutical compositions containing such compounds. The compounds are useful in treating diseases and conditions mediated by TEAD, such as cancer.