Chemistry Skill

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Expertise in Chemical Reactions  

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Grignard Reaction

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. Double Grignard reaction is carried out in Montelukast Sodium to directly convert ester to its respective alcohol.

Friedel-Craft Reaction

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.

Catalytic Hydrogenation

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. Different in situ generated intermediates are monitored by GC. andcyanogroup 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

Cyanation

Cyanations are carried out in homogeneous and biphasic media. A proper method of effluent treatment has been developed for destruction of residual cyanide.

Bromination

Bromination of the active methylene group is a tricky reaction as there is a possibility of formation of dibromoderivatives.Suitable reaction condition at commercial scale have been developed for the optimum formation of the desired product.

Wolff-Kishner Reduction

Ketone of one of the intermediates is reduced using hydrazine hydrate and sodium hydroxide.Appropriate temperature conditions have been established at commercial scale to get optimum yield of the product.

Michael Reaction

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.

Carbon Homologation

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.

Intermolecular Cyclization

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.

Intramolecular Cyclization

A highly concentrated solution of an N-alkylated aromatic ketone derivative is forced to undergo intramolecularcyclisation in the presence of a transition metal salt to yield an indole derivative.

Ketalisation

Acid catalysedketalisation of a highly sensitive 1,3-diol ester under very mild experimental conditions provides a very pure crystalline intermediate.

Deketalisation

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.

Condensation

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.

Amide Formation

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.

Methylation

Process for methylation using dimethylsulfate as a reagent has been commercialized incorporating all safety aspects.

Hydrolysis

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.

Esterification

Conditions for esterification have been developed on commercial scale using different acids to give high purity product minimizing effluent and pollution load.

Reduction

Ester of one of the intermediate is reduced to alcohol using sodium borohydride activated with aluminum chloride. Process for ketone reduction to form a hydroxy group has been commercialized using sodium borohydride.

Stereoselective Reduction

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 cisdiol derivatives.

Heck reaction

The Heck reaction (also called the Mizoroki-Heck reaction) is the chemical reaction of an unsaturated halide (or triflate) with an alkene and a strong base and palladium catalyst to form a substituted alkene. Together with the other palladium-catalyzed cross-coupling reactions, this reaction is of great importance, as it allows to do substitution reactions on planar centers. It is named after the American chemist Richard F. Heck.

Morepen's Strengths - Chemistry

 

Amino acid Coupling
Acetylation/ Alkylation Reaction
Dapagliflozin (DP04)
Fexofenadine (D01, D05)
Saxagliptin (SX02)
Amino acid Coupling
Saxagliptin (SX01)
Sitagliptin (SG05)
Amine/ Hydroxy Deprotection
Atorvastatin (AT09A)
Candesartan (CS06)
Dapagliflozin (DP05)
Fexofenadine (D07)
Linagliptin (LG04)
Olmesartan (OL05)
Rosuvastatin (RT11)
Saxagliptin (SX04, SX05)
Sitagliptin (SG06))
Bromination Reaction
Atorvastatin (ATN02)
Rosuvastatin (RTN08)
Chiral Synthesis
Montelukast (MT07)
Sitagliptin (SGN06)
Condensation Reaction
Candesartan (CS05)
Fexofenadine (D10)
Linagliptin (LG02, LG03)
Olmesartan (OL02, OL04)
Cyanation Reactions
Loratadine (L05)
Saxagliptin (SX03)
Esterification
Fexofenadine (D09)
Montelukast (MTS05)
Ester hydrolysis
Atorvastatin (AT10)
Desloratadine (DCL/DH)
Fexofenadine (D12)
Montelukast (MTN11, MK11)
Olmesartan (OL03)
Rosuvastatin (RT12)
Friedel Craft Reaction
Fexofenadine (D06, DN05)
Loratadine (L07)
Grignard reaction
Fexofenadine (D0)
Loratadine (L08, LN08)
Montelukast (MTN02, MT08)
Hetero Cyclization
Atorvastatin (AT08)
Loratadine (LH09)
High pressure Hydrogenation
Atorvastatin (AT07)
Sitagliptin (SGN06)
Voglibose (VG05)
Nucleophilic Substitution
Loratadine (L01, L10, LH10)
Montelukast (MTN10, MK10)
Rosuvastatin (RT10)
Oxidation Reaction
Fexofenadine (D08)
Loratadine (L04)
Rosuvastatin (RT08, RTS06)
Reduction Reaction
Fexofenadine (D04, D11)
Loratadine (L3)
Vilsmair Haack Reaction
Montelukast (MTN06)