C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
260/489, 260/595
C07C 213/04 (2006.01) C07C 69/157 (2006.01)
Patent
CA 1260008
ABSTRACT OF THE DISCLOSURE A new process is provided herein for the preparation of the therapeutically-useful product 2,3-cis-1,2,3,4-tetrahydro-5-[(2- hydroxy)-5-tert,butylamino)propoxyl]-2,3-naphthalenediol, a compound having Formula (I) Image (I) 5,8-Dihydro-1-naphthol-1-acetate is first oxidized with N- methylmorpholine-N-oxide and a catalytic amount of osmium tetroxide to form cis-2,3-dihydroxy-1,2,3,4-tetrahydro- naphthalene-5-acetate, which is then converted with acetone to the corresponding acetonide having the Formula (V). That acetonide is reacted by a phase-transfer technique in a sodium hydroxide solution - dichloromethane mixture in the presence of a quarternary alkyl ammonium halide with epichlorohydrin to form a compound having the Formula (VI): Image (V) (VI), Abstract of the Disclosure (Page 2) Reacting such compound having Formula (VI) with tert.butylamine gives the acetonide of the compound of Formula (I), which in turn is hydrolyzed to a compound having Formula (I). The compound having Formula (1), is known by the generic name NADOLOL, which has .beta.-adrenergic-blocking properties, and thus is useful in the treatment of hypertension.
464989
Farmos - Yhtyma Oy
Mcfadden Fincham
LandOfFree
Process for the preparation of 2,3-cis-1,2,3,4-... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Process for the preparation of 2,3-cis-1,2,3,4-..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Process for the preparation of 2,3-cis-1,2,3,4-... will most certainly appreciate the feedback.
Profile ID: LFCA-PAI-O-1253955