Physiologically active substance K-252, process for producing same and pharmaceutical composition containing same

Claim 1

A physiologically active substance K-252 having the following physico-chemical properties: State: Light yellow, columnar crystal Melting point: 262°-273° C. (decomposed) Specific rotation: [α] D 20 =-23.2° C. (C=0.5, CHCl 3 ) Solubility: Readily soluble in chloroform, acetonitrile, acetone, dioxane, tetrahydrofuran and pyridine; soluble in ethanol, methanol, 1-propanol, ethyl acetate and n-butanol; insoluble in water, 2-propanol, etc. Color reaction: Positive to reactions with each, iodine and ninhydrin; negative to reaction with ferric chloride and Rydon-Smith reaction Ultraviolet absorption spectrum (ethanol): FIG. 1 Infrared absorption spectrum (KBr): FIG. 2 Mass Spectrum: The mass spectrum of the present substance gives the following molecule ions and fragment ions: 467, 424, 406, 364, 337, 321 Elemental analysis: H4.47, C69.08, N8.79% (as found); H4.52, C69.37, N8.98% (as calculated as C 27 H 21 N 3 O 5 ) PMR spectrum (CDCl 3 ): δ(ppm) 2.16 (3H, s), 2.81 (1H, dd, J=4.9, 14.2), 3.44 (1H, dd, J=7.1, 14.2), 4.08 (3H, s), 4.61 (1H, d, J=17.0), 4.69 (1H, d, J=17.0) 5.46 (1H, brs), 6.79 (1H, dd, J=4.9, 7.1) 7.0-7.6 (6H, m), 7.7-8.0 (2H, m), 8.87 (1H, d, J=7.8) CMR spectrum (CDCl 3 ): δ(ppm) 22.8, 42.4, 45.9, 53.3, 84.9, 85.7, 99.5, 107.2, 114.2, 114.7, 116.4, 117.8, 119.3, 120.5, 120.7, 122.1, 123.9, 124.9, 125.0, 125.5, 125.8, 129.0, 132.3, 136.8, 140.3, 172.5, 173.5.