3970-21-6Relevant academic research and scientific papers
ANALOGS OF PYRIMIDINE NUCLEOSIDES. 14. SYNTHESIS AND ANTITUMORIGENIC ACTIVITY OF ALKOXYALKYL DERIVATIVES OF 5-FLUOROURACIL
Karpeiskii, M. Ya.,Mikhailov, S. M.,Tsieminya, A. S.,Ziderman, A. A.,Kravchenko, I. M.,et al.
, p. 1176 - 1179 (1980)
A number of alkoxyalkyl derivatives of 5-fluorouracil were synthesized by alkylation of 2,4-bis(trimethylsilyl)-5-fluorouracil with α-chloro ethers or by the addition of 5-fluorouracil to vinyl ethers.It was established that the synthesized compounds are capable of increasing the lifetimes of mice with L-1210 leukemia and La hemocytoblastosis.The UV and NMR spectra of the synthesized compounds are presented.
BREAST CANCER RESISTANCE PROTEIN (BCRP) INHIBITOR
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Page/Page column 13, (2010/02/14)
The invention provides a drug which inhibits BCRP. A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1): [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (-NHCOCH3 group), a cyano group (-CN group), a formyl group (-CHO group), -COOR1 (R1 is hydrogen or C1-C4 alkyl) , -O(CH2)nCOOR2 (n=1-7: R2 is hydrogen or C1-C4 alkyl) , -OOCCH2CH2COOR3 (R3 is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., -OP(O) (OH)2) or a salt thereof, a sulfate group (i.e., -OSO3H) or a salt thereof, a glycopyranosyl group or a salt thereof, a phosphate ester of a glycopyranosyl group or a salt of the ester, a sulfate ester of a glycopyranosyl group or a salt of the ester, or a piperidinopiperidinocarbonyloxy group], an ester thereof, or a salt thereof.
Process for the preparation of halogenated ethers
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, (2008/06/13)
The invention relates to a process for the preparation of compounds of formula I STR1 wherein R is mono- or disubstituted lower alkyl, the substituents being selected from halogen and lower alkoxy, with the proviso that said substituents are not present at the carbon atom of the lower alkyl radical R linking the group R to the remainder of the molecule of formula I; R1 is hydrogen, lower alkyl, phenyl or phenyl-lower alkyl; and X is chloro or bromo; which comprises reacting an acetal of formula II, STR2 wherein R and R1 are as defined above, with at least one compound of formula R2 --X, wherein R2 is hydrogen or X--SO, in which last mentioned case the reaction mixture must contain a catalytically effective amount of N,N-di-lower alkyl-lower alkanoylamide(s) and wherein X is as defined with respect to the compounds of formula I. The compounds of formula I are useful intermediates, suitably for the synthesis of pharmaceutical or fungicidal compounds.
An easy access to homopropargylic ethers
Guedin-Vuong, Denis,Nakatani, Yoichi
, p. 245 - 252 (2007/10/02)
Chloromethyl ethers, obtained from alcohols, formaldehyde and HCl, react regioselectively, as shown previously in one case by L.Miginiac, with allenyl aluminium reagents derived from propargyl bromides and aluminium, to give homopropargyl ethers.No evidence for the presence of allenyl ethers was obtained in the cases described.This condensation is used to obtain a protected acetylenic synthon 1, required for the synthesis of an ecdysteroid analogue (1).
THE SYNTHESIS OF PGF1α BY RE-STRUCTURING OF CASTOR OIL
Ranganathan, D.,Ranganathan, S.,Mehrotra, M. M.
, p. 1869 - 1876 (2007/10/02)
Castor oil has been transformed - via methyl ricinoleate - to PGF1α by strategy wherein 16 of the 18 carbons of the castor oil backbone are incorporated in the C-20 PGF1α, involving, inter alia, a novel procedure for the regiospecific functionalisation of terminal olefins, a novel degradation of aldehyde to lower acid and strategies useful for the generation of the highly functionalised prostanoid system, which specially illustrate the utility of MEM protecting group in diverse types of chemical transformations.Additionally, this work describes the preparation of synthons having potential utility and the synthesis of novel homo-PGF1α.
