Expertise in Chemical Reactions
Specific technology has been developed to synthesize Grignard reagent by in
situ activation of magnesium. With the activated magnesium, Grignard reagent
can be formed at low temperatures. Facilities are there to generate Grignard
reagent in refluxing too. Non-aqueous cooling medium is used in the condenser
for safety reasons.
Facilities are adequate for in situ generation of the acid chloride required
for Friedel-Craft Reaction. HPLC method is developed to monitor in situ
formation of acid chloride through derivatisation since acid chloride is not
stable under reverse phase HPLC conditions.
Hydrogenator of 2000 ltrs capacity is available for hydrogenation. Pyrophoric
palladium carbon is handled in a safe manner. Reductive amination coupled with
debenzylation is carried out in one-pot reaction. Differences in situ generated
intermediates are monitored by GC. and Cyanogroup of a highly substituted ester
derivative is reduced to a primary amino group in the presence of Raney nickel
at a pressure of 6-8 Kg/cm2
Cyanations are carried out in homogeneous and biphasic media. A proper method
of effluent treatment has been developed for destruction of residual cyanides.
Bromination of the active methylene group is a tricky reaction as there is a
possibility of formation of dibromo derivatives.Suitable reaction condition at
commercial scale have been developed for the optimum formation of the desired
Ketone of one of the intermediates is reduced using hydrazine hydrate and
sodium hydroxide.Appropriate temperature condition have been established at
commercial scale to get optimum yield of the product.
Dialkylation of primary amine is carried out with ethyl acrylate and the
Resulting dialkylated product is used in subsequent step without purification.
Excellent technology has been stabilized on commercial scale to obtain quality
dialkylamine without purification under Michael reaction.Similarly technology
for synthesizing highly substituted 1,4-diketones involving the Michael
addition of aromatic aldehydes to activated olefins under the Steller catalytic
condition have been successfully scaled up.
Low temperature experimental conditions involving coupling of n-butyl
lithium/diisopropylamine generated carbanion derived from esters with hydroxy
substituted esters leading to ß-ketoester via a 2-carbon homologation have been
scaled up.A similar transformation involving the reaction of a dianion
generated from a ß-ketoester (in the presence of sodium hydride/n-butyllithium
at low temperatures) with an aldehyde provides advanced pharmaceutical
intermediate via a 4-carbon homologation methodology.
Acid assisted experimental conditions have been developed for the cyclization
of tetrasubstituted 1,4-diketones with a highly functionalized primary amine in
a ternary solvent system to provide an advance pyrrole derivative in a
reasonably good yield.
A highly concentrated solution of an N-alkylated aromatic ketone derivative is
forced to undergo intramolecular cyclisation in the presence of a transition
metal salt to yield an indole derivative.
Acid catalysed ketalisation of a highly sensitive 1,3-diol ester under very
mild experimental conditions provides a very pure crystalline intermediate.
Under extremely controlled and mild acidic conditions,
protected ketal functionality of a highly sensitive substituted heterocyclic
compound is selectively deprotected in the presence of tertiary butyl ester
group to provide an advanced intermediate.
A high yield synthesis of an activated trisubstituted olefin via condensation
of a ß-ketoester derivative and aromatic aldehydes has been standardized under
very mild conditions.
Substituted ß-ketoester is reacted with aromatic amines under refluxing
conditions to provide the amide derivative in high purity which is then
straightway used in the next stage without further purification.
Process for methylation using dimethylsulfate as a reagent has been
commercialized incorporating all safety aspects.
Nitrile of one of the intermediate is hydrolysed to carboxylic acid giving
almost quantitative yield at the commercial scale. In another intermediate
ester is hydrolysed to give carboxylic acid.
Conditions for esterification have been developed on commercial scale using
different acids to give high purity product minimizing effluent and pollution
Ester of one of the intermediate is reduced to alcohol using sodium borohydride
activated with aluminium chloride. Process for ketone reduction to form a
hydroxy group has been commercialized using sodium borohydride.
Very low temperature experimental conditions (-90ºC to 100ºC) have been
utilized to carry out stereoselective reduction of hydroxy substituted
ß-ketoester in the presence of boranes and sodium borohydride to synthesize cis
1,3-diol derivatives. Higher temperatures lead to the formation of trans 1,3
diols in higher proportions which cannot be easily separated from the cis diol
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