Bracco Industria Chimica, S.p.a.

Syntex LLC

Bracco Industria Chimica Societa Per Azioni

Davide Pitre

Ernst Felder

Hans Zutter

Compounds for use in non-ionic X-ray contrasting materials having the formula ##STR1## in which (H0).sub.2-3 alkyl is 1,3-dihydroxyisopropyl, 2,3-dihydroxypropyl or 1,3-dihydroxy-2-hydroxymethylisopropyl,

Derivatives of 2,4,6-triiodo-isophthalic acid, processes for their

Novel, radio-opaque compounds comprising water-soluble bis-[N-{3,5-bis-(hydroxyalkylaminocarbonyl)-2,4,6-triiodo-phenyl}-N-(.alph a.-hydroxyacyl)-amino]-alkanes are disclosed for use as X-ray contrast agents. These compounds are relatively simple to synthesize, possess low toxicity and have good stability as well as resistance to hydrolysis. Methods for preparation and use of the compounds are also disclosed.

New derivatives of 2,4,6-triiodo-isophthalic acid, proceses for their

3-Alkoxy-2-alkyl-propionic acid derivatives are prepared by catalytic hydrogenation of the acrylic acid analogs. The latter are obtained by CO treatment of lower alkyl esters of alkanoic acids having 3-6 carbon atoms in the presence of alkali metal methylate and condensation of the resulting 2-formylalkanoic acids or their alkali metal enolates with compounds of the formula X--(CH.sub.2).sub.m --Z wherein X is Cl, Br, or OH, and Z is Cl, Br, I, alkyl- or arylsulfonyl, or OH.

Method of preparing a 3-alkoxy-2-alkyl-propionic acid ester derivative

The subject of the invention is a process for resolving mixtures of (+)- and (-)-6-methoxy-.alpha.-methyl-2-naphthaleneacetic acid into the enantiomers thereof, characterized in that N-methyl-D-glucamine [=1-deoxy-1-(methylamino)-D-glucitol] is used as the resolving agent, so that the 6-methoxy-.alpha.-methyl-2-naphthaleneacetic acid is converted into the corresponding diastereoisomeric N-methyl-D-glucamine salt pair which, because of very different solubilities, can be separated easily and completely with high yield.

Process for the resolution of (+)- and

.alpha., .omega.-BIS-[5-(DIHYDROXYALKYL) AMINOCARBONYL-3-HYDROXYACYL-AMINO-2,4,6-TRIIODO-BENZOYL-AMINO]-OXAALKANE COMPOUNDS OF THE FORMULA ##STR1## wherein R.sub.1 is ##STR2## R and R' are hydrogen or methyl, R.sub.2 is dihydroxyalkyl having 3 or 4 carbon atoms,

Water-soluble, non-ionizing, radiopaque compounds and contrast

Compounds of the formula ##STR1## wherein R is (C.sub.m H.sub.2m O.sub.n)--OH, m being 2, 3, or 4, and n being 0 or 1, are effective and well tolerated as X-ray contrast agents in lymphography, hepatography, bronchography, cystography, and hysterosalpingography.

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Milan, Italy

Davide Pitre