114079-44-6Relevant articles and documents
Interrupting the Barton?McCombie reaction: Aqueous deoxygenative trifluoromethylation of o-alkyl thiocarbonates
Liu, Zhi-Yun,Cook, Silas P.
, p. 808 - 813 (2021)
The site-selective trifluoromethylation of aliphatic systems remains an important challenge. This work describes a light-driven, copper-mediated trifluoromethylation of O-alkyl thiocarbonates. The reaction provides broad functional group tolerance (e.g., alkyne, alkene, phenol, free alcohol, electron-rich and -deficient arenes), thereby offering orthogonality and practicality for trifluoromethylation. A radical organometallic mechanism is proposed.
NOVEL HETEROAROMATIC AMIDE DERIVATIVE AND MEDICINE CONTAINING SAME
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Paragraph 0415; 0423, (2021/07/24)
A compound selectively inhibiting Nav1.7 over Nav1.5 is provided. A heteroaromatic amide derivative or salt thereof showing high efficacy for various diseases associated with Nav1.7 such as pain, represented by the general formula (I) [wherein, X1-X2 is N-C or C-N, Y1 , Y2, Y3 and Y4 are -CH2-, -CR4aH- or -O- and so on, Z1 is-O- and so on, ring A is a 3- to 7-membered monocyclic aromatic ring and so on, R1a and R1b are a hydrogen atom or a halogen atom and so on, R2 is a hydrogen atom and so on, R3a, R3b and R3c are a hydrogen atom or an optionally substituted C1-C6 haloalkyl group and so on, R4a, R4b and R4c are, an optionally substituted C1-C6 haloalkyl group or C1-C6 haloalkoxy group and so on, R5a is a hydrogen atom and so on, R5a and R5b together form -CH2O- and so on, R6a and R6b are a hydrogen atom and so on, n is 1 or 2.].
NOVEL PHARMACEUTICAL COMPRISING HETEROAROMATIC AMIDE DERIVATIVE OR SALT THEREOF
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Paragraph 0753-0755, (2021/09/17)
PROBLEM TO BE SOLVED: To provide a compound useful for treating or preventing disease associated with voltage-dependent sodium channel (Nav1.7) such as disease involving a pain, disease involving an itch, autonomic nerve-associated disease, or a pharmaceutical composition thereof. SOLUTION: The present disclosure provides a compound illustrated by the following formula, and a pharmaceutical composition containing the same. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
The evolution of a stereoselective synthesis of the C1-C16 fragment of bryostatins
Ball, Matthew,Baron, Anne,Bradshaw, Ben,Dumeunier, Rapha?l,O'Brien, Matthew,Thomas, Eric J.
, p. 9650 - 9681 (2016/10/22)
The development of a synthesis of the C1-C16 fragment of bryostatins in which the key step is a stereoselective oxy-Michael reaction used to assemble the cis-2,6-disubstituted tetrahydropyran with the exocyclic alkene already installed, is described. Foll
Mild deprotection of PMB ethers using tert-butyl bromide
Rival, Nicolas,Albornoz Grados, Arantxa,Schiavo, Lucie,Colobert, Fran?oise,Hanquet, Gilles
, p. 6823 - 6826 (2015/11/27)
A convenient and high yielding method for the cleavage and scavenging of p-methoxybenzyl protecting group of several alcohols using tert-butyl bromide in refluxing acetonitrile is described. Under these mild conditions other protecting groups such as acid sensitive allyl, benzyl, and Me3CPh2Si ethers, or isopropylidene acetals were unchanged. Interestingly, a selective alkoxy-PMB cleavage was observed in the presence of a PMB phenoxy ether.
ARYLOXYALKYLENE-SUBSTITUTED HYDROXYPHENYLHEXYNOIC ACIDS, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS A MEDICAMENT
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Page/Page column 53, (2012/01/14)
The invention relates to aryloxyalkylene-substituted hydroxyphenylhexynoic acid derivatives, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R
A mild and efficient cleavage of tert-butyldimethylsilyl (TBS) and tetrahydropyranyl (THP) ethers using a catalytic amount of TBPA+ {radical dot} Sb Cl6-
Xu, Yanfen,Tang, Shouchu,Han, Junjie,She, Xuegong,Pan, Xinfu
, p. 3634 - 3637 (2008/09/19)
A mild and efficient method for the deprotection of the TBS and THP ethers is described. A wide variety of TBS ethers as well as THP ethers can be easily deprotected to the corresponding parent hydroxyl compounds by employing a catalytic amount of tris(4-bromophenyl)aminium hexachloroantimonate (TBPA+ {radical dot} Sb Cl6-) in methanol at room temperature in good yield.
Cyanation of alcohols with diethyl cyanophosphonate and 2,6-dimethyl-1,4-benzoquinone by a new type of oxidation-reduction condensation
Masutani, Kouta,Minowa, Tomofumi,Hagiwara, Yoshiaki,Mukaiyama, Teruaki
, p. 1106 - 1117 (2007/10/03)
Cyanation of various alcohols by a new type of oxidation-reduction condensation is described. Primary alkyl diphenylphosphinites, 2,6-dimethyl-1,4-benzoquinone (DMBQ), and diethyl cyanophosphonate gave the corresponding nitriles in high yields. During the above experiment on cyanation of 4-phenylbutan-2-ol, the unexpected formation of a mixture of nitrile and isocyanide was observed. After careful examination of the reaction conditions, selective synthesis of isocyanides from secondary alcohols was successfully accomplished by the use of zinc oxide (ZnO) as an additive. Reaction of tertiary alcohols provided the corresponding isocyanides exclusively in the absence of an additive. Cyanation of optically active alcohols was tried in order to clarify the stereochemistry of this reaction, and the reaction was thus proved to proceed with the inversion of configuration.
Deprotection of acetals and silyl ethers using a polymer-supported π- acid catalyst: Chemoselectivity and polymer effect
Tanaka, Nobuyuki,Masaki, Yukio
, p. 1960 - 1962 (2007/10/03)
A polymeric dicyanoketene acetal (DCKA), prepared from a styrene monomer bearing dicyanoketene acetal functionality, was found to be an effective and recyclable catalyst in the chemoselective deprotection of acetals and silyl ethers. A remarkable acceleration accountable for the polymer effect was observed.
Synthesis and transannular Diels-Alder reaction of a 13-membered macrocyclic triene. A synthetic approach towards the tricyclic part A.B.C.[6.6.5] of the veratrum alkaloids
Quimpere,Ruest,Deslongchamps
, p. 132 - 140 (2007/10/02)
The syntheses of the acyclic triene cis-trans-trans (3Z,9Z,11E)-13-chloro-3-methoxy-1,1,7,7-tetrakis(methoxycarbonyl)-4- methyltrideca-3,9,11-triene (25), and the corresponding trans-cis-trans (3Z,9E,11E) isomer 37, and trans-trans-trans (3Z,9E,11E) isomer, 46, are described. Compounds 25 and 37 furnished in good yield 13-membered macrocyclic compounds (3Z,9Z,11E)- and (3Z,9E,11Z)-3-methoxy-1,1,7,7-tetrakis(methoxycarbonyl)-4- methylcyclotride-ca-3,9,11-triene (26) and (38) which led to tricyclic compound (cis-anti-cis)-2-methoxy-4,4,11,11-tetrakis(methoxycarbonyl)-1- methyl-tricyclo[7.4.0.02,6]tridec-7-ene (27) by transannular Diels-Alder reaction. Macrocyclization of trans-trans-trans chloride 46 was not successful.
