- Reducing dehalogenating method of organic halogenated compound
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The invention discloses a reducing dehalogenating method of an organic halogenated compound. The reducing dehalogenating method comprises: mixing an organic halogenated compound R-X, a non-noble metalpromoter, a sulfide and an alkali, and carrying out a reducing dehalogenating reaction to obtain a reducing product R-H, wherein R is at least one selected from alkyl and aryl, and X is at least oneselected from iodine, bromine and chlorine. According to the present invention, the types and the ratio (especially the specific type of the promoter) of various raw materials used in the reducing dehalogenating reaction, the corresponding reaction conditions and the like are researched and improved, such that the problems of use of highly-toxic or expensive reagent, poor tolerance of the group, narrow application range of the substrate and the like in the prior art can be effectively solved.
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Paragraph 0099; 0100; 0102; 0124; 0129; 0130
(2019/02/10)
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- 17-substituted steroids useful in cancer treatment
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Compounds of the general formula (1) STR1 wherein X represents the residue of the A, B and C rings of a steroid, R represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, R 14 represents a hydrogen atom and R 15 represents a hydrogen atom or an alkyl or alkoxy group of 1-4 carbon atoms, or a hydroxy or alkylcarbonyloxy group of 2 to 5 carbon atoms or R 14 and R 15 together represent a double bond, and R 16 represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, in the form of the free bases or phannaceutically acceptable acid addition salts, are useful for treatment of androgen-dependent disorders, especially prostatic cancer, and also oestrogen-dependent disorders such as breast cancer.
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- Photochemical Behavior of Δ4-3-Oxo, Δ5-7-Oxo, and Δ1-3-Oxo Steroids in Concentrated Acid Solution
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Irradiation with UV light of 5α-androst-1-en-3-one (9) in concentrated sulfuric acid leads to 15 and 16; similarly 4a-methyl-4a,5,6,7,8,8a-hexahydronaphthalen-2(1H)-one (10) gives 17 and 18.The formation of the four products is rationalized in terms of a photochemically induced 1,2-alkyl shift to the positively charged positions of the starting carbenium ions.On the other hand, irradiation under the same conditions of 4, 8, 7, and 11 yields, quantitatively, unchanged starting material, while the analogous bicyclic compound Δ1,9-10-methyl-2-octalone (1) has been reported to yield photorearrangement products.The lack of reactivity of 7 and 11 can be explained according to the proposed mechanism for the photorearrangement of 1.In the case of 4 and 8, the presence of the steroid rings C and D prevents the photorearrangement, but the mechanistic explanation of this effect cannot be determined from the present experimental data.
- Lupon, Pilar,Canals, Francesc,Iglesias, Arsenio,Ferrer, Joan C.,Palomer, Albert,et al.
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p. 2193 - 2198
(2007/10/02)
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- Steroids. Part 32. Configurational Analysis of 16-Methyltestosterone Derivatives
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The four possible isomers of 16-methylandrost-5-ene-3β,17-diol (1)-(4) have been converted into the corresponding 17-hydroxy-16-methylandrost-4-en-3-ones (5)-(8).The steric structures of the resulting epimers have been determined by 13C and 1H n.m.r. spectroscopy; thereby the exact configurational correlation of several 17-hydroxy-16-methylandrost-4-en-3-ones, reported in the literature, have been established.
- Schneider, Gyula,Mesko, Eszter,Hackler, Laszlo,Dombi Gyoergy,Zeigan, Dieter,Engelhardt, Guenter
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p. 1597 - 1600
(2007/10/02)
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- PHOTOREDUCTION DES ESTERS CARBOXYLIQUES DANS L'HEXAMETHYLPHOSPHORTRIAMIDE (HMPT)
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Use of HMPT as solvent in photochemistry allows efficient photoreductions.Alkyl esters and especially non absorbing alkyl acetates are photoreduced in excellent yields into alkanes.In the latter case, a protonating agent is necessary.Numerous examples illustrate the generality and convenience of the reaction.This photoreduction involves an electron transfer from HMPT to ester.
- Portella, C.,Deshayes, H.,Pete, J. P.,Scholler, D.
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p. 3635 - 3644
(2007/10/02)
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- Identification by gas chromatography mass spectrometry of intermediates in the aromatization of modified C19 steroids by human placental microsomes
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Analogs of 4 androstene 3,17 dione and testosterone were tested as substrates for the aromatizing enzyme complex of human placenta. Compounds modified in rings B, C, and D were found to be aromatized via a pathway similar to that postulated for 4 androstene 3,17 dione and testosterone, in which oxidation to the 19 hydroxy and 19 oxo (or corresponding gem diol) intermediates occurs. No evidence of additional intermediates was obtained.
- Braselton Jr,Orr,Engel
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p. 411 - 433
(2007/10/13)
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