Zambon S.p.a.

Zambon Group S.p.a.

Agrimont S.p.a.

Agrimont S.r.l.

Dario Chiarino

Davide Della Bella

Angelo Carenzi

Giancarlo Jommi

Mario Fantucci

Franco Pellacini

Gian Carlo Grancini

Roberto Pagliarin

Mauro Napoletano

Viviana Frigeni

Carlo Veneziani

Giovanni Camaggi

Giovanni Meazza

Giancarlo Grancini

Alberto Sala

Vittorio Ferrari

Uberto Teotino

Antonio Longo

Giancarlo Benelli

Replacement with fluorine of the primary hydroxy group of 1-phenyl-2-amino-1,3-propanediol compounds wherein the secondary hydroxy group and the amino group have been suitably protected. The reaction is carried out with an inorganic fluoride in a polyglycol. New oxazoline compounds particularly useful in said process.

Process for preparing 1-phenyl-2-amino-3-fluoro-1-propanols

Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X have the meanings reported in the description, can be used in compositions for agricultural use in particular as herbicides in the defense of useful crops from weeds.

Compositions having herbicidal activity containing N-alkyl-amides as

Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X have the meanings reported in the description, can be used in compositions for agricultural use in particular as herbicides in the defence of useful crops from weeds.

Replacement with fluorine of the primary hydroxy group of 1-phenyl-2-amino-1,3-propanediol compounds wherein the secundary hydroxy group and the amino group have been suitably protected. The reaction is carried out with an inorganic fluoride in a polyglycol. New oxazoline compounds particularly useful in said-process.

Process for fluorinating 1-phenyl-2-amino-1,3-propanediol compounds and

Intermediates of Formula ##STR1## where R is a methylthio, methylsulfoxy, methylsulfonyl or a nitro group; and

Intermediates for the preparation of

A diastereoselective process for the preparation of compounds of formula ##STR1## (wherein R and R.sub.1 have the meanings reported in the specification and the asterisks show the asymmetric carbon atoms) starting from the corresponding N-protected 2-amino-3-aryl-propan-1-ol is described. The compounds of formula I are intermediates useful for the synthesis of pharmacologically active peptides.

Diastereoselective process for the preparation of intermediates useful

Intermediates having the formula ##STR1## wherein R is --NO.sub.2, CH.sub.3 S--, CH.sub.3 SO--, or CH.sub.3 SO.sub.2 --, X.sub.1 is hydrogen, alkyl, haloalkyl, (substituted) phenyl or phenylalkyl and Y is F or --OSO.sub.2 R.sub.6 wherein R.sub.6 is methyl, trifluoromethyl, (substituted) phenyl naphthyl or pyridyl are disclosed.

2 Hydrocarbyl-4 substituted methyl 5 (4 substituted phenyl)-oxazolines

Compounds of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and n have the meanings reported in the specification, processes for their preparation and pharmaceutical compositions containing them as active ingredient are described. The compounds of formula I are inhibitor of enzymatic systems and they are useful in pharmaceutical field.

Peptides with pharmaceutical activity

A stereoselective process for the preparation of the compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, a and b have the meanings reported in the specification, is described. The compounds of formula I have a remarkable central analgesic activity and they are useful in the pharmaceutical field.

Stereoselective process for the preparation of 2-amino-ethanol

The blood level of orally administered N-acetylcysteine is substantially increased in a mammal when the N-acetylcysteine is administered in combination with tris(hydroxymethyl)aminomethane or a pharmaceutically acceptable salt thereof, in a molar ratio of about 1:0.8 to about l:l.2.

Method and composition for oral administration of N-acetylcysteine

Compounds of formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and n have the meanings reported in the specification, processes for their preparation and pharmaceutical compositions containing them as active ingredient are described. The compounds of formula I are inhibitors of enzymatic systems and they are useful in pharmaceutical field.

Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2 and Y have the meanings indicated in the description), a process for the preparation thereof and pharmaceutical compositions containing them as active ingredient are described. Compounds of formula I exhibit anto-serotonin activity.

Isoxazole containing compounds exhibiting anti-serotonin activity

Isoxazoles with nootropic activity

Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2, R.sub.3 and n have the meanings reported in the specification), their salts with pharmaceutically acceptable acids, process for their preparation and pharmaceutical compositions containing them are described. The compounds of formula I have a remarkable analgesic activity.

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Monza, Italy

Dario Chiarino