18187-31-0Relevant academic research and scientific papers
Methods for the total chemical synthesis of enantiomerically-pure 7-(2′-trimethylsilyl)ethyl camptothecin
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Page/Page column 14, (2014/05/20)
The present invention discloses and claims five (5) novel, highly efficient synthetic routes for the total synthesis of enantiomerically-pure (i.e., 99%) 7-(2′-trimethylsilyl)ethyl camptothecin (BNP1350; Karenitecin; Cositecan). These aforementioned synthetic schemes are the first to disclose the total syntheses of 7-(2′-trimethylsilyl)ethyl camptothecin using a highly novel direct, non-linear and convergent synthetic strategy which involves annealing the key C7-(trimethylsilyl)ethyl side chain-bearing A ring key synthons to an enantiomerically-pure tricyclic pyridone; rather than through the conventional methodology which incorporates the C7-(trimethylsilyl)ethyl side chain as the final synthetic step on a totally synthesized camptothecin parent compound. The current novel synthetic approaches reported herein since utilize desirably functionalized A-ring with preinstalled trimethyl silyl ethyl side chain, the aforementioned synthetic methodologies have a wider scope of making wide range of pharmaceutically relevant A-ring substituted BNP1350 analogs by substituting desirably functionalized nitro or protected amino phenyl carboxy A-ring as the starting material.
SILINANE COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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Page/Page column 52, (2008/06/13)
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them. The present invention is also directed to the use of these inhibitors in combination with a therapy that causes a deleterious immune response in patients receiving the therapy.
Photoprotective cosmetic compositions containing aromatic amide, sulphonamide or carbamate derivatives of acrylonitrile and novel aromatic amide, sulphonamide or carbamate derivatives of acrylonitrile
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, (2008/06/13)
Cosmetic compositions for topical use for protecting the skin and the hair, containing, in a cosmetically acceptable support, at least one compound of formula (1) or (2) in which X1 represents R3—(C═O)—, R3—SO2—
6-substituted-3,5-diamino-1,2,4-triazines as insecticides
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, (2008/06/13)
An insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of a 1,2,4-triazine compound of the formula STR1 wherein m is 0 to 12; n is 0 or 1; T is CH2, CH=CH, or C C; X is Si(CH3)2, C(CH3)2, CH(CH3), or O; or R is methyl, vinyl, cyclopentyl, phenyl, naphthyl, or a substituted phenyl of the formula: STR2 wherein Q, U, W, Y, Z, and R1, R2, R3, R4 are as defined herein; and methods of using the same.
Asymmetric synthesis of α-methylene-γ-butyrolactones fused to carbocyclic rings via the Hosomi reaction of chiral allylsilanes
Nishitani, Kiyoshi,Yamakawa, Koji
, p. 387 - 390 (2007/10/02)
Optically active α-methylene-γ-butyrolactones fused to five or six-membered carbocyclic ring were synthesized in 64-92% enantiomeric excess using the intramolecular Hosomi reaction of ω-formylated β-(chiral)alkoxycarbonylallylsilanes.
