3934-81-4Relevant articles and documents
Preparation method of dioxane-quinazoline derivative
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Paragraph 0040-0044, (2019/06/12)
The invention relates to a preparation method of a dioxane-quinazoline derivative and belongs to the field of medicine intermediate synthesis. Compared with a reported route, the route has the advantages that the procedures are much simpler and the overall yield is increased. An R group includes methyl, ethyl, propyl, isopropyl, methoxyethyl, methoxypropyl, N, N-dimethylaminopropyl, 3-pyrrolidinepropyl, tetrahydropyranyl, cyclopentanyl, 3-piperidine propyl and 3-morpholine propyl, wherein specific information is shown in the description.
Process development of the PDE4 inhibitor K-34
Yanagisawa, Arata,Taga, Masashi,Atsumi, Toshiyuki,Nishimura, Koichiro,Ando, Kyoji,Taguchi, Tsuyoshi,Tsumuki, Hiroshi,Chujo, Iwao,Mohri, Shin-Ichiro
experimental part, p. 376 - 381 (2012/02/01)
A short and practical synthesis of the PDE4 inhibitor K-34 (1) was developed. This synthesis was achieved in four steps and with a 58% overall yield. The unique spiro acetal was created with exceptionally high yield by utilizing the neighbor carboxylic acid assistance. This synthesis also features efficient ketone construction with 4-pyridinylmethyl anion 9 and ester 18, in which overreaction should be prohibited by quick in situ enolate formation. The overall synthesis was carried out under mild conditions and used a simple procedure suitable for large-scale production.
SELECTIVE DEMETHYLATIONS IN 2,3,4-TRIMETHOXYARYL CARBONYL COMPOUNDS
Kaisalo, Leena,Latvala, Anita,Hase, Tapio
, p. 645 - 648 (2007/10/02)
2,3,4-Trimethoxybenzaldehyde, -acetophenone and -benzoic acid give the corresponding 2,3-dihydroxy-4-methoxy compounds in good yield on treatment with BCl3.