156579-01-0Relevant academic research and scientific papers
An improved process for the large-scale preparation of antirheumatic agent MX-68
Maruyama, Noriaki,Shimizu, Hirohito,Sugiyama, Takashi,Watanabe, Masashi,Makino, Masashi,Kato, Masahiro,Shimizu, Makoto
, p. 883 - 888 (2004)
A large-scale preparation route of MX-68, a novel MTX derivative bearing a dihydro-2H-1,4-benzothiazine moiety and L-homogulutamic acid, is described. The original route that is a laboratory-scale synthesis for preclinical study has been improved. The improved process involves the following features: each step does not use haloalkane solvents, corrosive reagents, and chromatographic purification, and the formation of the major impurity at the final step is minimized. This improvement has enabled us to supply sufficient quantities of MX-68, which is required for both the toxicity test and the clinical study.
Synthesis of tritiated N-[4-(2,4-diaminopteridine-6-methyl)-3,4-dihydro-2H-1,4- benzothiazine-7-carbonyl]-L-homo glutamic acid (MX-68)
Matsuoka, Hiroharu,Kuroki, Toshio,Yano, Keiichi,Takeda, Yasuhisa
, p. 363 - 368 (2007/10/03)
Synthesis of tritiated N-[4-(2,4-diaminopteridine-6-methyl)-3,4-dihydro-2H-1,4-benzothiazine-7 -carbonyl]-L-homoglutamic acid, [9-3H,]MX-68 (3), is described. [9-3H1MX-68 (3) was prepared via tritiation at the carbonyl group in 2,4-bis(butanoylamino)-6-formylpteridine (7) with sodium borotritiide.
