Pharmaceutical research company synthesis

Computerized Aids to Organic Synthesis in a Pharmaceutical Research Company... 

This company founded in 1994, is a contract molecular biology and screening service company for the pharmaceutical, research, and clinical markets worldwide. Custom services include gene synthesis, DNA sequencing, site-directed mutagenesis, nucleic acid purification, and genotype/genetic analysis. 

Since that time, the pharmaceutical industry in the developed world has focused primarily on the synthesis of compounds for development as single agent prescription products. These efforts have required very substantial investments and, in the USA alone, investment in pharmaceutical research and development is probably close to 40 billion per year. In order to prevent the theft of a drug by an entity that has made no investment in the discovery and development research programme, companies have sought to protect their investments through the patent process. 

The problem of chiral synthesis is critical in making pharmaceuticals. Researchers at GlaxoSmithKline, AstraZeneca and Pfizer have examined 128 syntheses from their own companies and found that as many as half of the drug compounds made by their process R D groups are not only chiral but also each contains an average of two chiral centers [ 15 2]. To meet regulatory requirements, enantiomeric purities of 99.5% were found to be necessary. Biocatalysis is thus an essential tool for pharmaceutical research, and contributes to the development of more sustainable processes. 

In recent years, developments in high-throughput screening inspired many pharmaceutical companies to focus and rely on combinatorial chemistry, especially massive parallel synthesis, to find new lead structures. The employed chemistry is often simple and the concept depends on sheer numbers for success. The main research areas were heterocyclic and peptide chemistry, and the resulting structures often lacked complexity and diversity, and most importantly the chance to utilize the evolutionary advantage of natural products with their privileged structures. 

During the last decade the design of potent FTIs has been the focus at a significant number of pharmaceutical companies and academic research institutions, as tools to better understand biology or as cUnical candidates, and has led to the synthesis of thousands of highly active compounds (some of them have already been cited in the preceding sections). It will not be possible to exhaustively review all these inhibitors, but we will rather focus on key examples and compounds that have reached the cUnical development phase. 

Despite their low cost and abundant availability, the applications of monoterpenes as chiral synthons or building blocks for synthesis of chiral fine chemicals on an industrial scale have lagged far behind amino acids and carbohydrates. Most of the work in this area is related to multi-step total synthesis of complex natural products in laboratory scale. With the structures of new drug candidates in the research and development pipeline of pharmaceutical companies getting bigger and more complicated, the application of more sophisticated chiral building blocks such as the terpenes will... 

All the optically active terpenes mentioned in this chapter are commercially available in bulk (>kg) quantities and are fairly inexpensive. Although many of them are isolated from natural sources, they can also be produced economically by synthetic methods. Actually, two thirds of these monoterpenes sold in the market today are manufactured by synthetic or semi-synthetic routes. These optically active molecules usually possess simple carbocyclic rings with one or two stereo-genic centers and have modest functionality for convenient structural manipulations. These unique features render them attractive as chiral pool materials for synthesis of optically active fine chemicals or pharmaceuticals. Industrial applications of these terpenes as chiral auxiliaries, chiral synthons, and chiral reagents have increased significantly in recent years. The expansion of the chiral pool into terpenes will continue with the increase in complexity and chirality of new drug candidates in the research and development pipeline of pharmaceutical companies. 

Several small firms market more sophisticated equipment than the domestic microwave oven, and research departments in a number of pharmaceutical companies continue to work with the technology to aid their synthesis of APIs and their intermediates. Several microwave equipment companies70 are developing larger-scale equipment to produce kilogram quantities. Their systems are evolving to meet some of the needs identified by the earlier practioners such as ... 

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