101023-70-5Relevant articles and documents
A concise synthesis of isoxazole-based side chain of Micafungin
Rao, Pallavi,Hussain, Ismail,Rao, Venkataramanarao,Sen, Saikat,Oruganti, Srinivas
, p. 2180 - 2187 (2019)
A concise synthesis of key isoxazole-based side chain of Micafungin, an USFDA approved anti-fungal agent, has been delineated. The route design notably involves a one pot regioselective isoxazole construction from the corresponding aryl aldehyde and alkyne intermediates.
Facile One-Pot Transformation of Primary Alcohols into 3-Aryl- and 3-Alkyl-isoxazoles and -pyrazoles
Kobayashi, Eiji,Togo, Hideo
, p. 3723 - 3735 (2019/09/30)
Various primary alcohols were smoothly transformed into 3-aryl- and 3-alkylisoxazoles in good yields in one pot by successive treatment with PhI(OAc) 2 in the presence of TEMPO, NH 2 OH, and then NCS, followed by reaction with alkynes in the presence of Et 3 N. Similarly, various primary alcohols were smoothly transformed into 3-aryl- and 3-alkylpyrazoles in good yields in one pot by successive treatment with PhI(OAc) 2 in the presence of TEMPO, PhNHNH 2, and then NCS and decyl methyl sulfide, followed by reaction with alkynes in the presence of Et 3 N. Thus, both 3-aryl- and 3-alkylisoxazoles, and 3-aryl- and 3-alkylpyrazoles could be prepared from readily available primary alcohols in one pot under transition-metal-free conditions.
Discovery of novel 5-oxa-2,6-diazaspiro[3.4]oct-6-ene derivatives as potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonists for treatment of type 2 diabetes mellitus
Hirose, Hideki,Yamasaki, Takeshi,Ogino, Masaki,Mizojiri, Ryo,Tamura-Okano, Yumiko,Yashiro, Hiroaki,Muraki, Yo,Nakano, Yoshihide,Sugama, Jun,Hata, Akito,Iwasaki, Shinji,Watanabe, Masanori,Maekawa, Tsuyoshi,Kasai, Shizuo
, p. 4175 - 4193 (2017/07/05)
Somatostatin receptor subtype 5 (SSTR5) has emerged as a novel attractive drug target for type 2 diabetes mellitus. Starting from N-benzyl azetidine derivatives 1 and 2 as in-house hit compounds, we explored the introduction of a carboxyl group into the t
