A new method is reported for the conversion of azidoacids into lactams, via thioester formation and in situ azide reduction and cyclisation under high-dilution conditions; since the quantitative conversion of macrolactams to macrolactones has been shown to be feasible, this results in an indirect, alternative macrolactonisation procedure.
Omega-azido acids, alter activation of the carboxyl groups as mixed anhydrides, N3(CH2)nCOOCOAr (Ar = 3,5-dinitrophenyl or 2,4,6-trichlorophenyl), can be converted to macrolactams in good yields by treatment with Bu3P under high-dilution conditions; the presence of 4-dimethylaminopyridine improves slightly the yields. Amides and peptides can be readily obtained by this procedure.
INTRAVENOUS INFUSION DOSAGE FORM FOR PEMETREXED
申请人:Sun Pharmaceutical Industries Ltd
公开号:EP3470045B1
公开(公告)日:2020-09-02
[EN] INTRAVENOUS INFUSION DOSAGE FORM FOR PEMETREXED<br/>[FR] FORME POSOLOGIQUE DE TYPE PERFUSION INTRAVEINEUSE POUR LE PÉMÉTREXED
申请人:SUN PHARMACEUTICAL IND LTD
公开号:WO2019073482A1
公开(公告)日:2019-04-18
The present invention relates to an intravenous infusion dosage form comprising: an aqueous solution of pemetrexed or its pharmaceutically acceptable salt at a concentration ranging from 1.0 mg/ml to 20.0 mg/ml present in a multilayered flexible plastic infusion container, wherein the multilayered flexible plastic infusion container has an oxygen scavenger layer sandwiched between an outermost and an innermost layer of the container, the container being free of a polyamide and wherein the multilayered flexible plastic infusion container filled with the aqueous solution of pemetrexed is autoclavable.
Incorporation of La<sup>3+</sup>in an Organic Network. A Polyphenol-Derived Solid Brønsted-Base Catalyst
作者:Toshiyuki Saiki、Yasuhiro Aoyama
DOI:10.1246/cl.1999.797
日期:1999.8
Treatment of anthracenebisresorcinol 1 (a tetraphenol) with La(OiPr)3 in THF affords an amorphous 1:2 (14− to La3+) coordination polymer (La host). It catalyzes typical base-promoted reactions such as Michael, nitroaldol, and, less effectively, aldol reactions, where the insoluble catalyst (La host) can be readily recovered and repeatedly used.