7149-59-9Relevant academic research and scientific papers
PYRIMIDINE COMPOUNDS CONTAINING ACIDIC GROUPS
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Paragraph 1170; 1171, (2018/06/15)
The present disclosure relates to a class of pyrimidine derivatives having immunomodulating properties that act via TLR7 which are useful in the treatment of viral infections and cancers.
Preparation methods for 5-aminolevulinic acid hydrochloride and 5-aminolevulinic acid hydrochloride intermediate
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, (2018/09/11)
The invention discloses preparation methods for a 5-aminolevulinic acid hydrochloride and a 5-aminolevulinic acid hydrochloride intermediate. The preparation method for the 5-aminolevulinic acid hydrochloride intermediate comprises: (1) carrying out a reaction on a compound 2 and isopropylidene malonate in an organic solvent under the actions of an organic alkali and a condensing agent to obtain acompound 3; and (2) carrying out a reaction on the compound 3 in a C1-C4 alcohol solvent to obtain a compound 4, wherein R1 and R' are respectively and independently C1-C4 alkyl. The present invention further provides a method for preparing a 5-aminolevulinic acid hydrochloride by using the 5-aminolevulinic acid hydrochloride intermediate. According to the present invention, the intermediate product is basically solid and is easily crystallized and purified; and the method has characteristics of high yield, low production cost and easy operation, and is suitable for industrial production. Thecompounds 1, 2, 3 and 4 are defined in the specification.
BENZOXAZEPINE COMPOUND
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Page/Page column 26-27, (2010/11/08)
A compound represented by the formula [1]: wherein ring A and ring B each represent an optionally substituted benzene ring; ring C represents an optionally further substituted aromatic ring; R1 represents a lower alkyl group optionally substituted with an optionally substituted hydroxyl group; X1a represents a bond or optionally substituted lower alkylene; X1b represents a bond or optionally substituted lower alkylene; X2 represents a bond, -O- or -S-; X3 represents a bond or an optionally substituted divalent hydrocarbon group; Y represents an optionally esterified or amidated carboxyl group, or a salt thereof. The compound of the formula [I] is safer and has more potent lipid lowering activity such as squalene synthase inhibitory activity (cholesterol lowering activity) and triglyceride lowering activity, and thus it is a compound useful as an agent for preventing or treating hyperlipemia.
The reactions of diazo compounds with lactones. Part 1. Cyclopropanespiro-β-lactones from diketene: Synthesis and reactions
Murphy, Paul V.,O'Sullivan, Timothy J.,Geraghty, Niall W.A.
, p. 2109 - 2119 (2007/10/03)
The cyclopropanespiro-β-lactones 3, 4 and 12 can be prepared by the metal catalysed, or photochemically promoted decomposition reactions of diazocompounds in the presence of diketene. The thermal reactions of these compounds give a variety of products depending on the nature of the spirolactone; these include a furan 9a, 1,4-dicarbonyl compounds 18a-c and 19b, a pyranone 20b, furanones 21a, 21f and 22a and the enol 16. The boron trifluoride promoted reaction of a mixture of 3b and 4b gives a 13-ketoacid. Mechanisms are proposed for the formation of these products. The rearrangment of the cyclopropanespiro-β-lactones to furan-2(5H)-ones and furan-2-(3H)-ones 6-8, 21a, 21f, 22a and 24 is shown to be a general reaction that involves metal catalysis. A mechanism based on formation of a metallocycle by a novel insertion of the metal into the C-O bond of the β-lactone ring is proposed for this rearrangement. This accounts for the observed features of the reaction.
Niobium pentachloride-mediated novel homologation reactions using α-trialkylstannylmethyl-β-keto esters
Yamamoto, Makoto,Nakazawa, Misako,Kishikawa, Keiki,Kohmoto, Shigeo
, p. 2353 - 2354 (2007/10/03)
In the presence of niobium pentachloride (NbCl5), an α-trialkylstannylmethyl-β-keto ester is homologated to the corresponding γ-keto ester in good yield; the reaction mechanism is discussed.
Metal catalysed rearrangement of cyclopropanespiro-β-lactones to 2-furanones
Geraghty, Niall W. A.,Murphy, Paul A.
, p. 6737 - 6740 (2007/10/02)
The rearrangement of 5-oxo-4-oxaspiro[2.3]hexanes (cyclopropanespiro-β-lactones) to 2(5H)-furanones and 2(3H)-furanones is shown to be a general reaction which is promoted by metal catalysts. A mechanism is proposed, involving the novel insertion of a metal species into the O-C(β) bond of the β-lactone ring, which explains the basic features of the reaction, including its regioselectivity.
Preparation of γ-Substituted β-Oxoesters with a New Heterocyclic Synthon
Doleschall, Gabor,Seres, Peter,Kovacs, Attila
, p. 324 - 346 (2007/10/02)
Ethyl 2,5-dihydro-2,3-dimethyl-5-oxoisoxazole-4-carboxylate was alkylated and acylated via its potassium-salt generated by potassium t-butoxide under convenient conditions.Hydrolysis of the enamines obtained by the catalytic hydrogenation of the 3-alkylated/acetylated derivatives affords β-oxo and β,δ-dioxoesters, respectively.Hydrogenolysis of the 3-acyl derivatives allows the regiospecific synthesis of β-enamino-δ-oxoesters.
A NEW ENAMINE-SALT FOR THE SYNTHESIS OF γ-ALKYLATED ETHYL ACETOACETATE DERIVATIVES
Doleschall, G.
, p. 6339 - 6340 (2007/10/02)
A convenient method for the preparation of γ-alkylated ethyl acetoacetate from alkyl halides via a new isoxazole enamine-salts is reported.
AN IMPROVED SYNTHESIS OF 2-METHYL-4-(2'-CARBOXYETHYL)PYRROLE. POTENTIAL INHIBITORS OF PORPHOBILINOGEN DEAMINASE
Wilen, Samuel H.,Shen, DeKang,Licata, Joseph M.,Baldwin, Enoch,Russell, Charlotte S.
, p. 1747 - 1757 (2007/10/02)
Improved syntheses of 2-methyl-4-(2'-carboxyethyl)pyrrole (10) (49percent overall yield) and of several O- and S-containing β-(5-ring heterocyclic)-substituted propionic acid are described.Some of these compounds have been found to be inhibitors of porphobilinogen deaminase.
