103909-78-0Relevant articles and documents
Industrial synthesis of maxacalcitol, the antihyperparathyroidism and antipsoriatic vitamin D3 analogue exhibiting low calcemic activity
Shimizu, Hitoshi,Shimizu, Kazuki,Kubodera, Noboru,Mikami, Tetsuhiro,Tsuzaki, Kaname,Suwa, Hiroyuki,Harada, Koji,Hiraide, Akira,Shimizu, Motoki,Koyama, Kaichiro,Ichikawa, Yoshihide,Hirasawa, Daisuke,Kito, Yasushi,Kobayashi, Mio,Kigawa, Masaharu,Kato, Masahiro,Kozono, Toshiro,Tanaka, Hideki,Tanabe, Makoto,Iguchi, Masanori,Yoshida, Mitsutaka
, p. 278 - 287 (2012/12/24)
Maxacalcitol, the 22-oxa-derivative of 1α,25-dihydroxyvitamin D 3 and used currently as an antihyperparathyroidism and antipsoriatic drug, has been synthesized in seven chemical steps from 1α- hydroxydehydroepiandrosterone on the basis of our previously developed route. The present synthesis allows the production of the protected form of the penultimate intermediate in 26% overall yield in a kilogram scale reaction employing neither difficult reaction conditions nor chromatographic purification, having overcome all the difficulties involved in the previous route.