News of the Week is a will-o'-the-wisp. Nobody— outside of his immediate family— seems to know where he is or what he's up to at any given time. His communications with university of ficials usually have been channeled through his North Carolina lawyer. Journalists trying to track him down reported in October that he had sold his house and moved his family to France. Even NCFI director Fritz G. Will thought that was the case. Now, however, the story is that he and his family had only been on va cation, and they are currently resid ing in another home outside Salt Lake City. As C&EN went to press, Pons was expected to meet with university of ficials over the weekend to discuss future funding of his research. The only thing certain at this point is that the uncertainties of the cold fu sion saga will spill over into the new year. Ron Dagani
Amino acid fluorides to aid peptide synthesis A series of amino acid derivatives reactive enough to condense readily in high yields with other amino ac ids, but stable enough to have a long shelf life, has been invented by chemists at the University of Massa chusetts, Amherst [/. Am. Chem. Soc, 112, 9651 (1990)]. The new reagents may find use in peptide syntheses in the solid state or in solution. The reagents are N-9-fluorenylmethoxycarbonyl (FMOC) amino acid fluorides. Organic chemistry professor Louis A. Carpino made them by reacting FMOC-amino ac ids with cyanuric fluoride, which came from the reaction of cyanuric chloride with sodium fluoride in sulfolane. Carpino did the work with graduate student Dean SadatAalaee, postdoctoral fellow Hann Guang Chao, and undergraduate Robert H. DeSelms. The Amherst workers even made stable amino acid fluorides from tertbutyl derivatives of serine, threo nine, tyrosine, and aspartic and glu tamic acids, from a terf-butoxycarbonyl derivative of lysine, and from underivatized tryptophan. The cor6
December 24, 1990 C&EN
neered pharmaceuticals on the mar ket. Recommended for approval for CH 2 OC—NHCH. use in stemming infections related to Τ XH 2 OC(CH 3 ) 3 cancer therapies is a product called Neupogen, a granulocyte colony stimulating factor (G-CSF). It was de Fluorenylmethoxycarbonyl serine veloped by Amgen, a biotechnology acid fluoride ferf-butyl ether firm based in Thousand Oaks, Calif. The panel also delivered positive responding FMOC-amino acid chlo recommendations on granulocyterides either cannot be made or de macrophage colony stimulating fac compose within a short time during tor (GM-CSF), for treatment of bone marrow transplant patients. Hostorage. In demonstrations with FMOC- echst-Roussel of Somerville, N.J., amino acid fluorides, the Amherst and Immunex of Seattle, worked to chemists made the heptapeptide gether on development of GM-CSF, Val-Asp-Val-Leu-Leu-Ser-Tyr as the and will comarket the drug under FMOC terf-butylated form in 33% two different product names— yield by a continuous series of rapid Prokine and Leukine, respectively. solution condensations, without iso Although potentially competing lation of intermediates. Treatment products, GM-CSF and G-CSF cur first with tris(aminoethyl)amine and rently are targeted for different next with cresol gave the free hep treatment indications, and thus dif tapeptide. ferent size markets. The investment A second demonstration was sol research and management firm of id-phase preparation of 75 mg of Sanford C. Bernstein & Co. in New Ala-Asn-Lys-Gly-Phe-Leu-Glu-Glu- York City estimates the worldwide Val in a batch synthesizer. This non- market for immunoprotective CSFs apeptide represents amino acids one will reach $1 billion by 1994, with through nine of prothrombin. Addi U.S. sales contributing more than tion of each amino acid took 10 min half. U.S. sales of G-CSF by Amgen are projected to reach $240 million utes per cycle. Research Corp. Technologies, in 1994, while Hoechst-Roussel and Tucson, Ariz., will seek patent pro Immunex share $70 million in GMtection for the FMOC-amino acid CSF sales. fluorides and their use in peptide For Immunex, nine years old and synthesis. It also will negotiate li not yet profitable, this would be its censes for the university. first proprietary drug product Stephen Stinson (C&EN, Dec. 17, page 8). Although no patents have been awarded on GM-CSF, the company faces a po tential patent dispute with Genetics Institute, Cambridge, Mass. An in terference has been declared by the U.S. Patent & Trademark Office be A Food & Drug Administration ad tween pending patent applications visory panel has recommended that of the two companies. FDA clear two bioengineered immuHowever, the favorable outcome noprotective proteins for first-time in what was Immunex's expedited marketing. second appearance before the FDA The Biological Response Modifi panel puts the company one step ers Advisory Committee recom closer to marketing the product. The mended just over a week ago that firm filed its product license appli FDA approve two colony stimulat cation in February. Observers expect ing factors (CSFs), proteins that reg that the Immunex and Hoechstulate the growth and function of Roussel products will enter the mar white blood cells and thus enhance ket before that of Sandoz/Scheringthe body's immunological defenses. Plough, licensees of Genetics Insti FDA must complete its own review, tute, which filed an application with but, if approved, the new products FDA in January. will join the 12 genetically engi Ann Thayer
Immunoprotective drug approvals recommended
