Catalytic Synthesis of Heterocycles. V.¹ Dehydrocyclization of Anils to Nitrogen Heterocycles

Abstract

701 CORWIK HANSCH, D. G. CROSBY, 5 I r c~z s~ SADOSKI, ALBERT LEO AND DOVGI,AS PERCIVAL Vol. 7 3Anal. Calcd. for CloH130S4Cl: Cl, 14.8. Found: c1, 15.0.Of the two possible isomers, 2-chloro-4-dimethylaminobenzaldehyde had been prEpared before" by an unambiguous synthesis; m. p . 82 . The 3-chloro-compound was synthesized by the following method and was found identical (mixed in. p.'s of the aldehydes and the semicarbazones) with the above substance.o-Chlorodimethylaniline was prepared by heating ochloroaniline (13 g.), methyl alcohol (20 cc.) and concd. sulfuric acid (1 cc.) for 16 hours at 160-170" (sealed tube), addition of alkali, extraction with ether and fractional distil--____

Methoxy-Substituted 3-Formyl-2-phenylindoles Inhibit Tubulin Polymerization

“…They were recorded in DMSO- d 6 as solvent except where noted and are consistent with the assigned structures; values are given in δ units (ppm). The syntheses of the 2-phenylindoles 1a , 1b , 1c , 1d , 1e , 1f , 2a , and 2d , 5-methoxy-2-(4-methoxyphenyl)benzo[ b ]furan, 6-methoxy-2-(4-methoxyphenyl)benzo[ b ]thiophene, and ( Z )-2,3-bis(4-methoxyphenyl)propenal ( 5 ) have been described previously.…”

The Dehydrocyclization Reaction.

“…This reaction has also been conducted catalytically with chromium catalysts (58). Under these conditions at 550°C.…”

Scaffold and cell line based approaches for QSAR studies on anticancer agents

“…They have shown unexpected biological properties and became the basis for a whole number of innovative medicinal agents. [21][22][23][24][25][26] This technique is the most important tool used in analogue-based drug design and has been broadly used for the calculation of assorted properties like carcinogenicity, 27 ADME, 28 stability, 29 toxicity, 30,31 retention time 32 and other physicochemical properties apart from the biological activity. [7][8][9] Preparation of libraries based on natural products requires sophisticated and laborious synthetic sequences.…”

“…19,20 QSAR has become crucial for the molecular interpretation of biological properties. [21][22][23][24][25][26] This technique is the most important tool used in analogue-based drug design and has been broadly used for the calculation of assorted properties like carcinogenicity, 27 ADME, 28 stability, 29 toxicity, 30,31 retention time 32 and other physicochemical properties apart from the biological activity. [33][34][35][36] The QSAR method makes possible the theoretical prediction of structures with desired property values by combining the QSAR method with pattern recognition techniques.…”