79867-76-8Relevant academic research and scientific papers
Synthesis of functionalized and unfunctionalized olefins via cross and ring-closing Metathesis
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, (2008/06/13)
The invention is directed to the cross-metathesis and ring-closing metathesis reactions between geminal disubstituted olefins and terminal olefins, wherein the reaction employs a Ruthenium or Osmium metal carbene complex. Specifically, the invention relates to the synthesis of α-functionalized or unfunctionalized olefins via intermolecular cross-metathesis and intramolecular ring-closing metathesis using a ruthenium alkylidene complex. The catalysts preferably used in the invention are of the general formula wherein: M is ruthenium or osmium; X and X1 are each independently an anionic ligand; L is a neutral electron donor ligand; and, R, R1R6, R7, R8, and R9 are each independently hydrogen or a substituent selected from the group consisting of C1-C20 alkyl, C2-C20 alkenyl, C2-C20 alkynyl, aryl, C1-C20 carboxylate, C1-C20 alkoxy, C2-C20 alkenyloxy, C2-C20 alkynyloxy, aryloxy, C2-C20 alkoxycarbonyl, C1-C20 alkylthio, C1-C20 alkylsulfonyl and C1-C20 alkylsulfinyl.
Enhanced Antitumor Properties of 3'-(4-Morpholinyl) and 3'-(4-Methoxy-1-piperidinyl) Dervatives of 3'-Deaminodaunorubicin
Mosher, Carol W.,Wu, Helen Y.,Fujiwara, Allan N.,Acton, Edward M.
, p. 18 - 24 (2007/10/02)
Reductive N,N-dialkylation of daunorubicin with 2,2'-oxydiacetaldehyde and NaBH3CN occurred in two steps without interruption and with cyclization to form 3'-(4-morpholinyl)-3'-deaminodaunorubicin.This derivative retained the antitumor efficacy of doxorubicin against mouse leukemia P388 but at one-fortieth the dose; hence, it is the most potent anthracycline analogue synthesized so far.The 4-methoxy-1-piperidinyl derivative, similarly prepared with 3-methoxyglutaraldehyde, showed improved efficacy against P388, though at normal doses.Results with a series of analogues indicate that incorporation of the N in the new ring and the presence of an ether O at the 4-position are critical for enhanced activity.
Octahydro-1H-benzo[4,5]furo[3,2-e]-isoquinoline analgesic and narcotic antagonistic compounds
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, (2008/06/13)
Octahydro-1H-benzo[4,5]furo[3,2-e]isoquinoline compounds and processes for their manufacture are provided. The compounds correspond to the formula STR1 These compounds exhibit both analgesic and narcotic antagonistic properties, as well as low abuse liability.Novel intermediate compounds are also provided which have the formula STR2
