Big molecules , also called high molecular weight , HMW molecules, are mostly oligomers or polymers of small molecules or chains of amino acids. Thus, within pharma sciences, peptides , proteins and oligonucleotides constitute the major categories. Peptides and proteins are oligomers or polycondensates of amino acids linked together by a carboxamide group.  The threshold between the two is as at about 50 amino acids. Because of their unique biological functions, a significant and growing part of new drug discovery and development is focused on this class of biomolecules. Their biological functions are determined by the exact arrangement or sequence of different amino acids in their makeup. For the synthesis of peptides, four categories of fine chemicals, commonly referred to as peptide building blocks (PBBs), are key, namely amino acids (=starting materials), protected amino acids, peptide fragments and peptides themselves. Along the way, the molecular weights increase from about 10 2 up to 10 4 and the unit prices from about $100 up to $10 5 per kilogram. However, only a small part of the total amino acid production is used for peptide synthesis. In fact, L-glutamic acid , D, L-methionine , L-aspartic acid and L-phenylalanine are used in large quantities as food and feed additives. About 50 peptide drugs are commercialized. The number of amino acids that make up a specific peptide varies widely. At the low end are the dipeptides . The most important drugs with a dipeptide (L-alanyl-L-proline) moiety are the “-pril” cardiovascular drugs , such as Alapril (lisinopril), Captoril (captopril), Novolac (imidapril) and Renitec (enalapril). Also the artificial sweetener Aspartame (N-L-α-Aspartyl-L-phenylalanine 1-methyl ester) is a dipeptide. At the high end there is the anticoagulant hirudin , MW ≈ 7000, which is composed of 65 amino acids.
Our process design chemists rely on expertise with a variety of synthetic methodology and techniques for the highly efficient, selective assembly of APIs. Illustrative examples include asymmetric catalysis, phase transfer catalysis, classical resolution of racemates, organometallics (Li, Mg, Pd, Ru, Sn, B, Si, Al, Ti, Zr, etc.), solid phase techniques, and supercritical fluids and alternative clean reaction media. Our global teams are experienced in handling a diverse range of molecular targets, including prostaglandins, steroids, peptides, polymers, nucleosides, carbohydrates, and heterocycles.
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