ABSTRACT
An improved synthesis of the molecule SR 48692 is presented and its use as a neurotensin antagonist biological probe for use in cancer research is described. The preparation includes an number of enhanced chemical conversions and strategies to overcome some of the limiting synthetic transformations in the original chemical route.
Subject(s)
Neurotensin/antagonists & inhibitors , Pyrazoles/chemical synthesis , Quinolines/chemical synthesis , Cell Line, Tumor , Dose-Response Relationship, Drug , Humans , Male , Molecular Structure , Prostatic Neoplasms/drug therapy , Pyrazoles/chemistry , Quinolines/chemistryABSTRACT
The frequently overlooked benefits that considerably simplify and enrich our standard of living are most often hinged upon chemical synthesis. From the development of drugs in the ongoing fight against disease to the more aesthetic aspects of society with the preparation of perfumes and cosmetics, synthetic chemistry is the pivotally involved science. Furthermore, the quality and quantity of our food supply relies heavily upon synthesised products, as do almost all aspects of our modern society ranging from paints, pigments and dyestuffs to plastics, polymers and other man-made materials. However, the demands being made on chemists are changing at an unprecedented pace and synthesis, or molecular assembly, must continue to evolve in response to the new challenges and opportunities that arise. Responding to this need for improved productivity and efficiency chemists have started to explore new approaches to compound synthesis. Flow-based synthesis incorporating solid supported reagents and scavengers has emerged as a powerful way of manipulating chemical entities and is envisaged to become a core laboratory technology of the future.
Subject(s)
Chemistry, Organic/methods , Chemistry, Pharmaceutical/methods , Combinatorial Chemistry Techniques , Drug Design , Equipment Design , Indicators and Reagents/chemistry , Microscopy, Electron , Microwaves , Models, Chemical , Organic Chemicals , Oxazoles/chemistry , Technology, Pharmaceutical/methods , TemperatureABSTRACT
A two step synthesis of trifluoromethyl ketones from aldehydes is reported. A combination of polymer-supported reagents and sequestering agents were employed to effect the transformation without the need for chromatographic purification.
Subject(s)
Polymers/chemistry , Aldehydes/chemistry , Combinatorial Chemistry Techniques , Hydrocarbons, Fluorinated/chemistry , Indicators and Reagents , Ion Exchange Resins , Ketones/chemistry , Oxidation-ReductionABSTRACT
Sildenafil 1 (Viagra), a well known and commercially important pharmaceutical drug, has been prepared using polymer-supported reagents in a multi-step, convergent process resulting in a clean and efficient preparation without the need for conventional purification methods.
