Drug synthesis, generalized

D. Lednicer and L. A. Mitscher, The Organic Chemistry of Drug Synthesis Vols. 1—4, John Wiley and Sons, Inc., New York, 1977,1980, 1984,1990, for general references of partial synthesis of steroid dmgs. 

Ursodeoxycholic acid (ursodiol), which is found in large quantities in bear bile, and which elicits an intense bitter taste, has long been used in traditional Chinese medicine not only as a stomachic but also as a universal drug for the alimentary system.1 8 Currently, the drug is generally derived by chemical synthesis rather than from animals. 

The search for a general synthesis of enantio-merically pure non-biaryl atropisomers has been given added impetus by the discovery [26, 27] that the absolute configuration of some atropiso-meric amides affects their biological activity. The enantiomeric atropisomers 21 and 22 (Scheme 13) differed in activity at the tachykinin NK, receptor by a factor of 6-13, with 21 being the more active. Atroposelectivity must now be an important new consideration in drug synthesis. 

Constituents of foods are frequently natural and not synthetic. Synthesis of organic compounds for general use tend not to be as complicated. Drug synthesis is frequently lengthy since only a very specific molecular shape and charge distribution will give the desired pharmacological effect and this is often not available from a simple, easily accessible compound. 

Generally, solvates are undesirable as drug substances especially if the solvents used are not class III solvents (see per ICH guidelines for organic volatile impurities). However, the formation of solvates does occur frequently during drug synthesis and manufacturing. Solvates, as inclusion complexes, can retain their structure, even after the solvent is removed, washed, and dried under vacuum. Solvates also exhibit distinct physicochanical... 

This openness of academic laboratories obviously presents tremendous opportunities for unauthorized individuals to gain access to labs to steal chemicals and equipment. Since the terrorist attacks on September 11, 2001 and more generally in the past decade with the increase in illicit drug synthesis (particularly methamphetamines), there has been a heightened awareness nationwide about access to chemicals. Some laws and regulations (described below) have emerged that address this situation. Nonetheless, many academic labs and stockrooms are still relatively unsecure with regard to theft. 

Methods for direct introduction of tritium gas into a drug by synthesis generally involve catalytic hydrogenation, by either tritium addition to an unsaturated system or tritium replacement of a halogen 2 . Such reactions are usually conducted on a micro or semi-... 

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