In this paper, all mono-and di-alkylanilines are the N-alkylated compounds.

No abstract

The evolution and development of a commercially viable synthesis of fenleuton, a second-generation 5-lipoxygenase inhibitor, is discussed. Special emphasis is given to the challenges and operational issues encountered on scale-up in the pilot plant. Three separate processes were developed and scaled up, providing valuable information about operational parameters and physical characteristics of the drug substance. A novel displacement reaction was discovered and developed and was incorporated as the key transformation in the final manufacturing process.

Two-dimensional double quantum NMR and relayed correlation spectroscopy were used to complete the ' H assignments of a series of glycopeptide antiiiotics. The double quantum N M R experiments were particularly useful in assigning the complicated aromatic region of the spectra by identifying the coupled protons with small differences in chemical shifts, and simplifying the contour maps by selectively enhancing the crosspeaks corresponding to either the orthe(343 Hz) or mefa-(&= 2 Hz) coupled protons. In addition, from the double quantum NMR experiments, protons belonging to the same spin system were unambiguously identified, even though not directly coupled. The comectivities between remote nuclei belonging to the same network were also established through relayed correlation spectroscopy.