2028-12-8Relevant academic research and scientific papers
Intramolecular Influence of a Carboxylic Function on Platinium Blue Synthesis. A systematic Study of Complexes Originating from Acid Amides
Arrizabalaga, Philippe,Castan, Paule,Laurent, Jean-Pierre
, p. 4814 - 4818 (1984)
The use of acid amide as ligand for obtaining platinium blue has been investigated.While blue compounds are generally obtained by using the hydrolysis product of cis-dichlorodiammineplatinum(II) as platinum surce, with such ligands the reaction occurs very readily using potassium tetrachloroplatinate(II).The role of the carboxylic function which offers here a primary ligating site to platinum is evidenced.The compounds obtained have been characterized by UV-visible spectral measurments, Ce(IV) oxydative titration , ESR spectroscopy, and magnetic properties.Antitumoral activity toward leukemia L1210 and sarcoma 180 is reported for two of thesecompounds.As a first step for this antitumor study, these compounds have been found to be inactive toward Leukemia while they presnt intersting activity toward Sarcoma.
Modification of the Enantioselectivity of Biocatalytic meso-Desymmetrization for Synthesis of Both Enantiomers of cis-1,2-Disubstituted Cyclohexane by Amidase Engineering
Hu, Hui-Juan,Wang, Qi-Qiang,Wang, De-Xian,Ao, Yu-Fei
supporting information, p. 4538 - 4543 (2021/08/09)
Both enantiomers of cis-1,2-disubstituted cyclohexane have been obtained enantioselectively through engineered amidase-catalyzed desymmetrization of meso carbocyclic 1,2-dicarboxamides under mild condition. Based on the enzyme-substrate binding model sugg
Preparation method of 1,2,3,6-tetrahydrophthalimide
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Paragraph 0061; 0062; 0064; 0065; 0067; 0068, (2020/01/12)
The invention provides a preparation method of 1,2,3,6-tetrahydrophthalimide. The preparation method comprises the following steps: a) mixing 1,2,3,6-tetrahydrophthalic anhydride with an ammonia source, and carrying out a low-temperature reaction to obtain a reaction intermediate, wherein the temperature of the low-temperature reaction is 0-30 DEG C; and b) carrying out a dehydration ring-closurereaction on the reaction intermediate obtained in the step a) in the presence of a solvent, carrying out cooling and recrystallizing to obtain the 1,2,3,6-tetrahydrophthalimide. According to the preparation method provided by the invention, a step-by-step method is adopted, a ring-opening reaction and a ring-closure reaction are separated to reduce side reactions, and a conventional heating process is not carried out in the whole process, so the generation of viscous colloidal byproducts in a temperature range of 80-110 DEG C can be effectively avoided, and high selectivity is realized, thereby improving product purity; meanwhile, reaction operation in a solvent is simple, conditions are easy to control, and environment friendliness is achieved; the overall two-step yield can reach 95% orhigher; moreover, no waste gas is generated in the reaction process, and redundant ammonia gas can be recycled, so environmental production cost is greatly saved.
1,3-Diaryl-4,5,6,7-tetrahydro-2H-isoindole derivatives: A new series of potent and selective COX-2 inhibitors in which a sulfonyl group is not a structural requisite
Portevin,Tordjman,Pastoureau,Bonnet,De Nanteuil
, p. 4582 - 4593 (2007/10/03)
Novel tetrahydro-2H-isoindoles have been prepared and evaluated as inhibitors of the COX-2 isoenzyme. A 1,3-diaryl substitution on the central polycyclic ring system and absence of a sulfonyl moiety are the two structural features of this chemical series.
Rhodococcus rhodochrous IFO 15564-mediated hydrolysis of alicyclic nitriles and amides: Stereoselectivity and use for kinetic resolution and asymmetrization
Matoishi, Kaori,Sano, Akio,Imai, Nori,Yamazaki, Takahiro,Yokoyama, Masahiro,Sugai, Takeshi,Ohta, Hiromichi
, p. 1097 - 1102 (2007/10/03)
The stereocourse and the selectivity of the hydrolysis of alicyclic mono- and dinitriles and amides mediated by Rhodococcus rhodochrous IFO · 15564 has been examined. The stereochemistry of the substrates, as well as the nature of substituents and presence of double bonds in alicyclic rings greatly affected the rate of hydrolysis by nitrile hydratase and amidase. The rate difference between enantiomers or enantiotopic groups, in some cases, enabled kinetic resolution or asymmetrization. The highest enantioselectivity of amidase was observed in the hydrolysis of 5-benzoyloxy-3-cyclohexene-1- carboxamide (E>200), and both enantiomers of methyl 5-hydroxy-3-cyclohexene- 1-carboxylate thus became readily available.
STEREOCHEMICAL STUDIES 83. SATURATED HETEROCYCLES 76. PREPARATION AND CONFORMATIONAL STUDY OF PARTIALLY SATURATED 3,1-BENZOXAZINES, 3,1-BENZOXAZIN-2-ONES AND 3,1-BENZOXAZINE-2-THIONES
Bernath, Gabor,Stajer, Geza,Szabo, Angela E.,Fueloep, Ferenc,Sohar, Pal
, p. 1353 - 1366 (2007/10/02)
The cis- and trans-2-amino-4-cyclohexene-1-carboxylic acids 1 and 3 react with imidates to give the condensed-skeleton, bicyclic cis- and trans-pyrimidin-4-ones 8 and 9.The amino acids 1 and 3 were reduced to the cis- and trans-1,3-aminoalcohols 6 and 7, which were cyclized by means of imidates to the bicyclic tetrahydro-4H-3,1-benzoxazines 10 and 11, or were converted, via the corresponding carbamates 14 and 15 into the tetrahydro-4H-3,1-benzoxazin-2(1H)-ones 16 and 17.The 2-thioxo analogues 18 and 19 were prepared by cyclization of the dithiocarbamates obtained from the aminoalcohols 6 and 7 by treatment with carbon disulphide.The trans-aminoalcohol 7 and its saturated analogue reacted with p-chlorobenzaldehyde to furnish the hexahydro 13 and octahydro-4H-3,1-benzoxazine 13a, respectively. 1H and 13C NMR studies showed that, similarly to the earlier-investigated analogues containing oxygen or unsubstituted nitrogen at position 1, the synthesized cis isomers 8, 10, 16 and 18 occurred as the preferred conformer in the heterocyclic twist inverse form of N-inside type (quasiaxal C6-N bond) (B).In the trans isomers containing a saturated C-2 atom (13 and 13a), H-2 and H-6 are in cis relative positions.
