Synthon B.v.

Synthon IP Inc.

Synthon Bct Technologies, LLC

Theodorus H A Peters

Jacobus Maria Lemmens

Franciscus B G Benneker

Frantisek Picha

Hans Jan Hoorn

Pavel Slanina

Rolf Keltjens

Jiri Bartl

Jaroslav Pis

Radim Scigel

Frans Van Dalen

Peter F A Bakker

Johannes J Platteeuw

Amlodipine free base can be formulated into a convenient oral dosage form, especially a tablet, without excessive stickiness or tablet punch residue. The amlodipine free base can be crystalline Form I or a novel Form II. Methods of making and using the amlodipine free base are set forth.

Amlodipine free base

Olanzapine and salts thereof are made by a process that utilizes an N-formyl olanzapine intermediate of formula (4) or a salt thereof 

Synthesis of olanzapine and intermediates thereof

A derivative of amlodipine having the following formula is useful as a pharmaceutical, either alone or in combination with amlodipine, in treating angina and hypertension. 

Amide derivative of amlodipine

A derivative of amlodipine having the following formula is useful as a pharmaceutical, either alone or in combination with amlodipine, in treating angina and hypertension 

Optically impure tamsulosin including racemic tamsulosin can be resolved into optically pure (R)- or (S)-tamsulosin by the use of diastereomeric sulfonate salts of tamsulosin in a fractional crystallization technique. Racemic tamsulosin free base is a useful starting material for the resolution process and a method of obtaining the same in solid form, including two crystalline polymorphic forms, is also provided.

Process for resolution of tamsulosin and compounds, compositions, and processes associated therewith

Amlodipine and related analogues thereof are prepared by the following general reaction scheme:Rand Reach independently represent a C-Calkyl group. The process provides for the formation of compounds of formula (1) in good yield and purity. Further, the compounds of formula (1) can be used as calcium channel blockers or as reference standards or reference markers for checking the purity of amlodipine.

Process for making amlodipine, derivatives thereof, and precursors therefor

Amlodipine aspartate and amlodipine maleamide are used as reference standards or markers in determining the purity of amlodipine maleate substances and products.

Reference standards for determining the purity or stability of amlodipine maleate and processes therefor

A compound or composition comprising N-formyl paroxetine of formula (1) is useful as a pharmaceutical and as a synthetic intermediate. The N-formyl paroxetine can be an impurity in paroxetine substances and methods of assaying for such an impurity are also useful.

N-formyl derivatives of paroxetine

The synthesis of paroxetine can be made more convenient by using a solvent system comprising an aliphatic alcohol and a hydrocarbon co-solvent. The solvent system is used particularly in the hydrolysis of paroxetine phenylcarbamate and preferably uses butanol and toluene as the system.

Process for the production of paroxetine

Process for making amlodipine

Paroxetine salt compositions having improved stability are formed by controlling the pH to 6.5 or less. The compositions can be made with the aide of water without significant coloration problems. The paroxetine salts include paroxetine hydrochloride salts but preferably use paroxetine sulfonate salts such as paroxetine methane sulfonate.

Paroxetine compositions and processes for making the same

A derivative of amlodipine having the following formula is useful as a pharmaceutical, either alone or in combination with amlodipine, in treating angina and hypertension.

Lactonization of statins can be achieved using a lactonization agent that forms a hydrated complex with the produced water that is insoluble in the reaction solvent. By binding the produced water in an insoluble complex, the reaction is pulled to the lactone side, using mild conditions in short reactions times and with reduced risk of impurities.

Lactonization process

Tosylate salts are useful in purifying 4-(fluorophenyl)-3-carbinol-piperidines from the corresponding des-fluoro impurity. The purified compounds are advantageously used in paroxetine synthesis.

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Arnhem, Netherlands

Theodorus H A Peters