Preparation of 2,4-diarylquinolines and substituted dihydrobenz-[c]acridines by the condensation of certain c(α),o-dilithiooximes with 2-aminobenzophenones

C(α),O-Dilithiooximes were prepared in an excess of lithium diisopropylamide and condensed with several 2-aminobenzophenones, followed by acid hydrolysis of the oximes to the ketones, which then underwent cyclodehydration and linear dehydration to give substituted quinolines or dihydrobenz[c]acridines.     

Synthesis of the carbocyclic analogs of uracil nucleosides

Treatment of the required hydroxyl derivatives of cis-3-aminocyclopentanemethanol with 3-ethoxyacryloyl isocyanate gave N-(3-ethoxyacryloyl)-N′-[hydroxy- or dihydroxy(hydroxy-methyl)cyclopentyl]ureas. Cyclization of the ureas in dilute sulfuric acid afforded high yields of the carbocyclic analogs of uridine, 2′-deoxyuridine, and 3′-deoxyuridine. The uridine and 3′-deoxyuridine analogs were also obtained in good yields by cyclizing the ureas in concentrated aqueous ammonia. None of the three analogs showed activity in tests versus KB cells in culture or L1210 leukemia in vivo.     

Derivatives of 2,4-diamino-6-methylpteridine

Eighteen derivatives of 2,4-diamino-6-methylpteridine related to methotrexate and aminopterin have been prepared from 6-(bromomethyl)-2,4-pteridinediamine by nucleophilic displacement reactions. None of these compounds showed any antileukemic acitivity.     

Folic acid analogs. Modifications in the benzene-ring region. 5. 2′,6′-diazafolic acid

The synthesis of 2′,6′-diazafolic acid was accomplished by the condensation of 2-acetylamino-4(3H)pteridinone-6-earboxaldehyde (XIV) with diethyl N-[(5-amino-2-pyrimidinyl)carbonyl]-L-glutamate (XIII) followed by reduction of the anil double bond and alkaline hydrolylic cleavage of the N²-acetyl and ethyl ester protecting groups. Intermediate XIII was prepared by starling with 5-nitro-2-styrylpyrimidine (VI) and proceeding via 5-arnino-2-styrylpyrimidine (IX). The henzyloxycarbonyl derivative of IX was prepared and oxidized to the corresponding 5-benzyloxycarbonylaminopyrimidine-2-carboxylic acid (XI). The coupling of XI with diethyl L-glutamate followed by hydrogenolysis of the henzyloxycarbonyl function afforded the desired intermediate XIII. 2′,6′-Diazafolic acid was a potent inhibitor of Streptococcus faecium and displayed marginal activity against leukemia 1,1210 in mice.     

The carbocyclic analog of cytidine,synthesis and antineoplastic activity

The carbocyclic analog (VI) of cytidine was prepared from the carbocyclic analog (I) of uridine. The intermediate stages were a tetrabenzoyl derivative of I, the tribenzoyl derivative of the uridine analog, and the tribenzoyl 4-chloropyrimidinone obtained from the latter derivative. The cytidine analog (VI) is active against KB cells in culture and against L1210 leukemia in mice. In the initial tests against L1210 leukemia, the highest dose (200 mg./kg./day, q.d. 1-9), of three active doses, increased lifespan by 82% and showed no evidence of toxicity.     

Untersuchung von Fetten und ?len

Ohne Zusammenfassung     

The diffraction of elastic waves by an imperfect fusion bond

We consider diffraction by a semi-infinite crack located alonga fusion interface between two differing elastic media. Twotypes of crack, namely open and partially closed cracks, areinvestigated. An open crack is modelled by a stress-free contactboundary condition and a partially closed crack is modelledby a spring contact boundary condition. For the latter, thejump in the stress across the crack is assumed to be proportionalto the jump in the displacement across the crack. This situationarises in, for example, a K-weld where the fine grain of theparent material (for example, ferritic or forged austeniticsteel) is in stark contrast with the coarse-grained weld metal(for example, austenitic weld metal). In the metal weld thedirection of the grain axis varies through the metal. However,diffraction is a local phenomenon and so the austenitic steelis assumed to have a zonal axis so that it may be modelled bya transversely isotropic composite. The ferritic or forged austeniticsteel will be modelled as an isotropic material.     

Reactions of diazo derivatives of 5-membered heterocycles with hydrazines

Interaction of hydrazine or dimethylhydrazine with 5-diazoimidazole-4-carboxamide produced, presumably via tetrazenes, high yields of 5-azidoimidazole-4-carboxamide. In contrast, when semicarbazide reacted with either the diazoimidazole or the analogous diazo-1,2,3-triazole, the yield of the azidoheterocycle was low, and the yield of biurea, and presumably the aminoheterocycle, was high. 3-Azidopyrazole-4-carboxamide was obtained from a reaction of hydrazine with the diazopyrazole. Both azido and amino derivatives were formed from reactions of diazo-imidazole esters with hydrazine or thiosemicarbazide.