Visy J, Simonyi M
Central Research Institute for Chemistry, Hungarian Academy of Sciences, Budapest.
Chirality. 1989;1(4):271-5. doi: 10.1002/chir.530010405.
2,3-Benzodiazepines containing a centre of asymmetry at C-5 possess both central and helical chiralities, and the solution of their racemates contains four molecular species. The binding of these compounds to human serum albumin (HSA) was studied by affinity chromatography. The binding strength depended both on the steric orientation of the 5-ethyl substituent and on the conformation of the diazepine ring. Conformation P (defined by the positive sign of C-1-N-2-N-3-C-4 torsion angle) is favoured, while the quasiaxial orientation of the 5-ethyl substituent is not favoured by the albumin molecule.
在C-5位含有不对称中心的2,3-苯并二氮杂䓬同时具有中心手性和螺旋手性，其外消旋体溶液包含四种分子种类。通过亲和色谱法研究了这些化合物与人血清白蛋白（HSA）的结合。结合强度既取决于5-乙基取代基的空间取向，也取决于二氮杂䓬环的构象。构象P（由C-1-N-2-N-3-C-4扭转角的正号定义）更受青睐，而5-乙基取代基的准轴向取向则不被白蛋白分子所青睐。
