cas 38692-80-7, 3-BROMO-4-HYDROXYPHENYLACETIC ACID

Articles about 38692-80-7Total 9 be found

Novel total synthesis method of racemic tetrandrine
The invention discloses a novel total synthesis method of racemic tetrandrine, and belongs to the technical field of pharmaceutical chemical synthesis. 5-bromovanillin and 4-hydroxyphenylacetic acid which are low in price and easy to obtain are respectively used as starting materials to synthesize a compound 10, the compound 10 is used for synthesizing a compound 12 and a compound 14 through a simple route, and the two compounds are subjected to intermolecular and intramolecular Ullmann reaction to synthesize the racemic tetrandrine A. The key intermediates 12 and 14 are synthesized through the compound 10, the synthesis efficiency is greatly improved, the raw materials are utilized to the maximum extent, and the method is a racemic tetrandrine total synthesis route which is simplest in operation and lowest in cost so far.
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Paragraph 0029; 0071; 0078-0079; 0105; 0112-0113; 0138; ...

(2021/07/01)

Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin
As an extension of our analysis of the effect of halogenation on thiourea TRPV1 agonists, we have now modified selected 4-hydroxy(or 4-amino)-3- methoxyphenyl acetamide TRPV1 agonists by 5- or 6-halogenation on the aromatic A-region and evaluated them for potency for TRPV1 binding and regulation and for their pattern of agonism/antagonism (efficacy). Halogenation shifted the functional activity at TRPV1 toward antagonism with a greater extent of antagonism as the size of the halogen increased (I > Br > Cl), as previously observed for the thiourea series. The extent of antagonism was greater for halogenation at the 5-position than at the 6-position, in contrast to SAR for the thiourea series. In this series, compounds 55 and 75 showed the most potent antagonism, with Ki (ant) = 2.77 and 2.19 nM, respectively, on rTRPV1 expressed in Chinese hamster ovary cells. The compounds were thus ca. 40-60-fold more potent than 6′-iodononivamide.
Kang, Dong Wook,Kim, Yong Soo,Lim, Kwang Su,Kim, Myeong Seop,Pearce, Larry V.,Pavlyukovets, Vladimir A.,Tao, Andy K.,Lang-Kuhs, Krystle A.,Blumberg, Peter M.,Lee, Jeewoo
experimental part
p. 8092 - 8105
(2011/01/13)

N,N-DISUBSTITUTED AMINOALKYLBIPHENYL ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS
Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
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Page/Page column 14; 15

(2009/08/16)

2-(2-HYDROXYBIPHENYL-3-YL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE DERIVATIVES AS FACTOR VIIA INHIBITORS
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
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Page 83

(2008/06/13)

2-'5-(5-CARBAMIMIDOYL-1H-HETEROARYL)-6-HYDROXYBIPHENYL-3-YL!- CARBOXYLIC ACID DERIVATIVES AS FACTOR VIIA INHIBITORS
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders. Processes for preparing these inhibitors are also disclosed.
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Page/Page column 28

(2010/02/07)

2- [5- (5-carbamimidoyl-1H-heteroaryl)-6-hydroxybiphenyl-3-yl]-succinic acid derivatives as factor viia inhibitors
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders. Processes for preparing these inhibitors are also disclosed.
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(2008/06/13)

Synthesis and Properties of Optically Active Phenoxypropionates. Effect of Halogeno Substituent in the Core on Physical Properties
Chiral phenoxypropionates having halogenated 2,5-diphenylpyrimidine cores were synthesized and the effect of a halogeno-substituent on the physical properties such as mesomorphic behavior, spontaneous polarization (Ps) and response time (τ) were investigated.The introduction of a halogen atom to the phenyl ring of 2,5-diphenylpyrimidine core led to a decrease in the thermal stability of mesophases.The Ps values in the achiral host liquid crystal mixture were increased by introducing the halogen atom.However, response times were not improved. - Keywords: ferroelectric liquid crystal, phenoxypropionate, halogeno-substituent
Sugita, Shin-Ichi,Toda, Susumu,Yoshiyasu, Takashi,Teraji, Tsutomu
p. 399 - 406
(2007/10/02)

On the Synthesis of Tiliacora Alkaloids, II: Synthesis of the Asymmetrical Biphenyl Derivative
The biphenyl derivatives S-1 and S-3 were obtained by mixed Ullmann reaction of the phenylacetic esters 3, 4 and 5.Because they contain selectively removable protective groups for the carboxyl functions, S-1 and S-3 are proper intermediates for the constitution selective reaction with the former described asymmetrical dibenzo-1,4-dioxin derivative K.
Pachaly, Peter,Schaefer, Michael
p. 483 - 487
(2007/10/02)

Novel, racemic or nearly-racemic antibacterial bromo- and chloroquinols and γ-lactams of the verongiaquinol and the cavernicolin type from the marine sponge Aplysina (= Verongia) cavernicola
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D'Ambrosio,Guerriero,Pietra
p. 1484 - 1492
(2007/10/02)