74106-81-3Relevant articles and documents
XANOMELINE DERIVATIVES AND METHODS FOR TREATING NEUROLOGICAL DISORDERS
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Paragraph 0235, (2021/05/21)
Provided herein are compounds comprising compounds of formula (I) and/or salts thereof; wherein at least one of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 is fluorine, and the remainder are independently chosen from hydrogen and fluorine; and R14, R15, R16, R17, R18, R19, R20, R21, R22, and R23 are independently chosen from hydrogen and deuterium; with the proviso that when R1, R2, and R3 are fluorine, then at least one of R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 is fluorine or at least one of R14, R15, R16, R17, R18, R19, R20, R21, R22, and R23is deuterium. Also provided are medicaments comprising these compounds and methods for treating central nervous system disorders with the compounds and medicaments described herein.
METHOD FOR PRODUCING FLUORINATED COMPOUND
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Paragraph 0151; 0152-0157; 0163; 0164; 0165; 0166, (2019/03/14)
This invention solves the problem of providing an efficient, new method for producing a fluoromethylene-containing compound. The problem can be solved by a method for producing a compound represented by formula (1) or a ring-closed or ring-opened derivative of the compound, wherein R1 represents an organic group, RX represents hydrogen or fluorine, R2a, R2b, R2c, and R2d are the same or different, and each represents —Y—R21 or —N(—R22)2, or R2b and R2c may join together to form a bond, wherein Y represents a bond, oxygen, or sulfur, R21 represents hydrogen or an organic group, and R22, in each occurrence, is the same or different and represents hydrogen or an organic group; the method comprising step A of reacting a compound represented by formula (2), wherein X represents a leaving group, and other symbols are as defined above, with a compound represented by formula (3), wherein the symbols are as defined above, in the presence of a reducing agent under light irradiation.
Synthesis of 2, 2 - [...] acid ethyl ester method (by machine translation)
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Paragraph 0012; 0029-0031, (2018/04/01)
The invention relates to a method for synthesizing 2, 2 - [...] acid ethyl ester method, the glass in the reaction container, adding benzoin two thioether and 2, 6 - dimethyl - 1, 4 - dihydro - 3, 5 - pyridine dicarboxylic acid diethyl, replace the nitrogen glass after the air in the reaction container, adding butene and bromine two fluorine ethyl acetate, then adding solvent; the glass reaction container is placed on a blue light LED lamp or white light energy-saving lamp irradiation under 12 - 48 h, then remove the product in the solvent, adding petroleum ether product dissolved, adopts the 300 - 400 mesh silica gel as the stationary phase of column chromatography technology, wet in france type, in order to petroleum ether as eluent to elute, GC - MS detection product belt, and the collected [...] turns on lathe does, to get the. The method is simple in operation, solvent to the low quality requirement, can be corresponding to the multi-olefin, raw materials are easy, low cost, mild reaction conditions, and adopts a non-metal catalytic, preventing the metal residue. (by machine translation)
Studies toward the oxidative and reductive activation of C-S bonds in 2′-S-aryl-2′-thiouridine derivatives
Rayala, Ramanjaneyulu,Giuglio-Tonolo, Alain,Broggi, Julie,Terme, Thierry,Vanelle, Patrice,Theard, Patricia,Médebielle, Maurice,Wnuk, Stanislaw F.
, p. 1969 - 1977 (2016/04/05)
Studies directed toward the oxidative and reductive desulfurization of readily available 2′-S-aryl-2′-thiouridine derivatives were investigated with the prospect to functionalize the C2′-position of nucleosides. The oxidative desulfurization-difluorination strategy was successful on 2-(arylthio)alkanoate surrogates, while extension of the combination of oxidants and fluoride sources was not an efficient fluorination protocol when applied to 2′-S-aryl-2′-thiouridine derivatives, resulting mainly in C5-halogenation of the pyrimidine ring and C2′-monofluorination without desulfurization. Cyclic voltammetry of 2′-arylsulfonyl-2′-deoxyuridines and their 2′-fluorinated analogues showed that cleavage of the arylsulfone moiety could occur, although at relatively high cathodic potentials. While reductive-desulfonylation of 2′-arylsulfonyl-2′-deoxyuridines with organic electron donors (OEDs) gave predominantly base-induced furan type products, chemical (OED) and electrochemical reductive-desulfonylation of the α-fluorosulfone derivatives yielded the 2′-deoxy-2′-fluorouridine and 2′,3′-didehydro-2′,3′-dideoxy-2′-fluorouridine derivatives. These results provided good evidence of the generation of a C2′-anion through carbon-sulfur bond cleavage, opening new horizons for the reductive-functionalization approaches in nucleosides.
Process for Preparing Lubiprostone and Intermediate Therefor
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Paragraph 0159; 0160, (2017/05/12)
The present invention relates to a method for producing lubiprostone and an intermediate product used therefor. According to the present invention, the selective introduction of a protecting group onto corey lactone diol enables the production of lubiprostone in an efficient and economical way.
PROSTAGLANDIN SYNTHESIS AND INTERMEDIATES FOR USE THEREIN
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Page/Page column 6, (2010/04/23)
Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
Synthesis of Aryl &α,&α-Difluoroalkyl Ketones as Potent Inhibitors of Cholesterol Esterase
Lin, Gialih,Liu, Hsiao-Chien,Wu, Fang-Chen,Chen, Show-Jane
, p. 103 - 108 (2007/10/02)
Aryl α,α-difluoroalkyl ketones were synthesized from the reaction of ethyl α,α-difluoroacylate with aryl lithium at -78 deg C or from the coupling of aryl iododifluoromethyl ketone with 1-alkene in the presence of teterakis(triphenylphisphine)palladium(0).These compounds were potent inhibitors of pancreatic cholesterol esterase with Ki values in the range 15 μM-20 nM.
Nickel-Catalyzed Reaction of Iodofluoroacetates with Alkenes and Zinc: A Novel and Practical Route to α,α-Difluoro-Functionalized Esters and α,α,ω,ω-Tetrafluoro Diesters
Yang, Zhen-Yu,Burton, Donald J.
, p. 5144 - 5149 (2007/10/02)
Iododifluoroacetates 1a-c react with alkenes and zinc in the presence of nickel dichloride hexahydrate in THF at room temperature or 60 deg C to give the corresponding α,α-difluoro esters in good yields.The reaction is also applicable to alkenes containing a variety of functional groups such as trimethylsilyl, hydroxy, ketone, and ester moieties.The reaction of 1 works well with dienes; the products formed depend on the length of chain of the dienes. 1,8-Nonadiene and 1,5-hexadiene afford the α,α,ω,ω-tetrafluoro diesters, while 1,6-heptadiene gave a mixture of ethyl 2,2-difluoro-8-nonenoate (19) and the cyclopentyl-substituted α,α-difluoroester 20.When diallyl ether was used as a substrate, only the tetrahydrofuran derivative 21 was formed.The nickel-catalyzed reaction can be suppressed by p-dinitrobenzene and hydroquinone.A single electron transfer initiated radical mechanism is proposed.
16-Substituted prostaglandins
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, (2008/06/13)
A process for producing optically active 16-substituted prostaglandins and new 16-substituted prostaglandins produced thereby which are useful as cardiovascular agents and as agents for inducing labor in pregnant females and for the termination of pregnancy.
