C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 307/92 (2006.01) C07D 493/08 (2006.01) C07D 493/18 (2006.01)
Patent
CA 2354516
Intermediates for the preparation of himbacine exhibiting muscarinic M2 receptor antagonism, which are hydronaphtho[2,3-c]furan derivatives represented by general formula (1) or intermediates for the preparation thereof: wherein R1 is lower alkyl or aralkyl; R2 is hydrogen, lower alkyl or aralkyl; R3 and R4 together represent oxygen or methylene, or alternatively R4 is hydroxyl, lower alkoxy, aralkyloxy or lower acyloxy, with R3 being hydrogen; R5 and R6 together represent oxygen, or alternatively R6 is hydroxyl, lower alkoxy, aralkyloxy or lower acyloxy, with R5 being hydrogen; and either of the broken lines is a single bond and the other thereof is a double bond, or alternatively both are single bonds.
L'invention concerne des intermédiaires servant à la préparation d'himbacine en tant qu'antagoniste du récepteur muscarinique M2. Ces intermédiaires sont des dérivés d'hydronaphto[2,3-c]furane de la formule générale (1) ou des intermédiaires destinés à la préparation desdits dérivés. Dans ladite formule, R¿1? est alkyle inférieur ou aralkyle; R¿2? est hydrogène, alkyle inférieur ou aralkyle; R¿3? et R¿4? forment ensemble oxygène ou méthylène, ou bien R¿4? est hydroxyle, alcoxy inférieur, aralkyloxy ou acyloxy inférieur, R¿3? étant hydrogène; R¿5? et R¿6? forment ensemble oxygène, ou bien R¿6? est hydroxyle, alcoxy inférieur, aralkyloxy ou acyloxy inférieur, R¿5? étant hydrogène; et l'une ou l'autre ligne brisée est une double liaison, ou bien l'une et l'autre sont une liaison simple.
Ishiwata Akihiro
Katoh Tadashi
Takadoi Masanori
Terashima Shiro
Borden Ladner Gervais Llp
Kyorin Pharmaceutical Co. Ltd.
Sagami Chemical Research Center
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