Water soluble tin(IV)-porphyrins, trans-dihydroxy-5,10,15,20-tetra(N-methyl-4′-pyridiniumyl)porphyrinate tin (IV) (Sn(IV)TMPyP(OH)2) was successfully synthesized in high yield (90%) through one-pot process in water at room temperature by treating the parent free base (H2TMPyP) with Sn(II)Cl2. R...
A tetrel bond can be defined as an interaction between any electron donating moiety and a group 14 element acting as Lewis acid. Experimental and theoretical research on this interaction has rapidly grown in recent years. A reason for that is related to the fact that it can be easily exploited t...
The double addition of bis(trimethylsilyl) ketene acetals [R1, R2 = CH3, –(CH2)5–] to pyridine N-oxide promoted by triflic anhydride under mild conditions generates N-[(trifluoromethane)sulfonyl-1,2-dihydropyridine-2,4-dicarboxylic acids 2a–b. Subsequent reaction of these acids upon iodolacto...
2-(Trimethylsilyl)ethanol as a new alcohol equivalent has been employed for copper-catalyzed coupling of aryl iodides. Using mild reaction conditions, it has been observed that substituted phenols and phenols with sensitive functional groups can be readily prepared.
In this paper, new chitosan (CS) coated magnetic iron oxide nanoparticles (MNPs) supported manganese Schiff-base complex was designed, synthesized and screened as an efficient, reusable nanocatalyst by the three-component reaction of various aldehyde derivatives with trimethylsilyl cyanide and 2...
A novel series of methylsulfonyl phenyl derivatives has been designed and synthesized to evaluate their COX-2 inhibitory activity along with anti-convulsant potential. In-vitro evaluation revealed that two compounds MTL-1 and MTL-2 appeared as most potent and selective COX-2 inhibitors in the en...
Contrary to the literature, the reaction of 3-bromothiochroman-4-one with sodium acetate in acetic acid gives a dimeric spirothioindoxyl (whose crystal structure has been determined) which, after bromination and then heating in pyridine yields “vinylenethioindigo”.
The synthesis of 3-[3/4-(2-aryl-2-oxoethoxy)arylidene]chroman/thiochroman-4-one derivatives (1–34) and evaluation of their anticancer activities were aimed in this work. Final compounds were obtained in multistep synthesis reactions using phenol/thiophenol derivatives as starting materials. For...
A highly enantioselective synthesis of (S)-3-aminomethyl-5-methylhexanoic acid 1 (Pregabalin) is reported. The key step of the synthesis is a quinine-mediated ring opening of 3-isobutylglutaric anhydride with cinnamyl alcohol. A Curtius rearrangement and subsequent deprotection provides 1 in hig...
Main chain chiral poly(methacrylate)s have been synthesized by controlled reversible addition–fragmentation chain transfer (RAFT) copolymerization of chiral monomer Boc-l-alanine methacryloyloxyethyl ester (Boc-l-Ala-HEMA, A) with Boc-d-alanine methacryloyloxyethyl ester (Boc-d-Ala-HEMA, B) and...
A simple and efficient method for the chemoselective N-Boc protection of the amine moiety in a variety of compounds is described using di-tert-butyl dicarbonate and guanidine hydrochloride as an organocatalyst in ethanol at 35–40 °C. Selective mono-N-Boc protection of diamines and chemoselecti...
A sensitive and specific radioimmunoassay is described for plasma and urinary levels of [D-Ser(tBu)]6des-Gly-NH210 ethylamide (buserelin).No appreciable cross-reaction (
An efficient stereoselective route to polyhydroxy-α-amino acids 7a-f was developed by exploiting N-tert-butoxycarbonyl-2-(tert-butyldimethylsiloxy)pyrrole as a glycine anion equivalent.
BackgroundActivity of nomegestrol acetate (NOMAC), levonorgestrel (LNG), drospirenone (DRSP), dienogest (DNG) and progesterone on human steroid receptor transactivation was investigated. Ovulation inhibition by NOMAC, LNG and progesterone was tested.
The efficacy and safety of a new monophasic oral contraceptive, norgestimate/ethinyl estradiol, containing the third-generation progestin, norgestimate (250 μg), and ethinyl estradiol (35 μg), are reviewed. Norgestimate/ethinyl estradiol demonstrates excellent contraceptive effica...
The metabolism of the progestogen oral contraceptive norgestimate has been studied in vitro using human intestinal mucosa and human liver microsomes. Metabolites have been separated using radiometric high-performance liquid chromatography (HPLC) and identified by co-chromatography with authentic...
This is a review of publications from January 2015 to December 2015 on sex hormones and related compounds. This chapter covers estrogens (diethylstilbestrol, estradiol and derivatives, conjugated estrogens, tamoxifen), progestins (cyproterone, desogestrel, drospirenone, etonogestrel, gestodene, ...
The androgenic and the progestational activity of norgestimate (NORG) and levonorgestrel (LNG) were compared in two animal studies. During a Hershberger test in immature castrated male rats and a pregnancy maintenance test in pregnant rats, NORG and LNG were administered subcutaneously at severa...
The progestational activity of norgestimate (NORG), levonorgestrel-oxime (LNG-oxime) and levonorgestrel (LNG) were compared in a pregnancy maintenance study in rats. The compounds were administered subcutaneously to pregnant rats at several doses, blood samples were collected repeatedly, and the...
A new line of research to enhance the performance of concrete under adverse (harsh) and normal (air cured) curing conditions is presented. A crystallising hydrophobic admixture and curing agents were added to fresh concrete to improve its resistance against severe environmental conditions. A two...
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