Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1994-09-12
1996-12-03
Trinh, Ba K.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
549372, 564153, 564155, 564158, C07D31906, C07D23367
Patent
active
055809936
ABSTRACT:
A process for the preparation of Iopamidol and 5-amino-2,2-dialkyl-1,3-dioxanes of formula ##STR1## wherein R and R.sub.1 are the same or different and represent a straight or branched C.sub.1 and C.sub.2 alkyl group or together with the carbon atom to which they are bonded, form a C.sub.5 -C.sub.6 cycloaliphatic ring; comprising the transformation of a 2,2-dialkyl-1,3-dioxane-5-carboxylic acid ester of formula ##STR2## wherein R.sub.2 represents a straight or branched C.sub.1 -C.sub.2 alkyl group, a phenyl optionally substituted by nitro groups or a benzyl; by treatment with ammonia into the corresponding amides and the subsequent rearrangement of the latter into the compounds of formula I, by treatment with a hypohalogenite. The resultant ketals may be used as is, or be converted to 2-amino-1,3-propanediol, and reacted with 5-amino-2,4,6-triiodo-isophthalic acid dichloride or, alternatively,L-5-(2-acetoxy-propionylamino)-2,4,6-triido-isophthalic acid dichloride, to produce Iopamidol.
REFERENCES:
patent: 4978793 (1990-12-01), Quirk et al.
Nardi Antonio
Villa Marco
Trinh Ba K.
Zambon Group S.p.A.
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