37470-46-5Relevant articles and documents
Active Site Binding Is Not Sufficient for Reductive Deiodination by Iodotyrosine Deiodinase
Ingavat, Nattha,Kavran, Jennifer M.,Sun, Zuodong,Rokita, Steven E.
, p. 1130 - 1139 (2017)
The minimal requirements for substrate recognition and turnover by iodotyrosine deiodinase were examined to learn the basis for its catalytic specificity. This enzyme is crucial for iodide homeostasis and the generation of thyroid hormone in chordates. 2-
Pd-Catalyzed ipso, meta-Dimethylation of ortho-Substituted Iodoarenes via a Base-Controlled C-H Activation Cascade with Dimethyl Carbonate as the Methyl Source
Wu, Zhuo,Wei, Feng,Wan, Bin,Zhang, Yanghui
supporting information, p. 4524 - 4530 (2021/05/04)
A methyl group can have a profound impact on the pharmacological properties of organic molecules. Hence, developing methylation methods and methylating reagents is essential in medicinal chemistry. We report a palladium-catalyzed dimethylation reaction of ortho-substituted iodoarenes using dimethyl carbonate as a methyl source. In the presence of K2CO3 as a base, iodoarenes are dimethylated at the ipso- and meta-positions of the iodo group, which represents a novel strategy for meta-C-H methylation. With KOAc as the base, subsequent oxidative C(sp3)-H/C(sp3)-H coupling occurs; in this case, the overall transformation achieves triple C-H activation to form three new C-C bonds. These reactions allow expedient access to 2,6-dimethylated phenols, 2,3-dihydrobenzofurans, and indanes, which are ubiquitous structural motifs and essential synthetic intermediates of biologically and pharmacologically active compounds.
Imidazole-containing condensed tricyclic compound and application thereof
-
Paragraph 0114, (2018/03/01)
The invention discloses an imidazole-containing condensed tricyclic compound adopting the structure as shown in the formula (I) or pharmaceutically acceptable salts, stereisomers or prodrug molecules thereof. The imidazole-containing condensed tricyclic compound has the IDO1 activity regulation function, can enhance T-cell activation through blocking immune checkpoints IDO1, is used for treating IDO1-mediated immunosuppression, and therefore, can become an effective medicine for treating malignant tumors. When used together with checkpoint protein anti-body drugs or other anti-cancer drugs, the imidazole-containing condensed tricyclic compound can enhance the anti-cancer effect. Meanwhile, the imidazole-containing condensed tricyclic compound has the potential of effectively treating IDO1 abnormity related immunosuppressive diseases and has a high application value.
CuLi2Cl4 catalysed cross-coupling strategy for the formal synthesis of the diterpenoid (+)-subersic acid from (?)-sclareol
Wu, Qiangyong,Wang, Peiqiang,Zhou, Bin,Hua, Sikai,Ren, Jiangmeng,Zeng, Bu-Bing
, p. 394 - 397 (2017/08/07)
A CuLi2Cl4-catalysed regioselective cross-coupling is used in a key step leading to the concise synthesis of (+)-subersic acid with an overall yield of 25.7% from commercially available (-)-sclareol. The coupled product 15-(2-methoxy-5-carbomethoxy)phenyl-labda-8(9),13Ediene was obtained in 62% yield under CuLi2Cl4 conditions starting from 2-iodo-4-carbomethoxyanisole and 15-acetoxy-labda-8(9),13Ediene. These were derived from 4-hydroxybenzoic acid and (-)-sclareol respectively. The 15-(2-methoxy-5-carbomethoxy)phenyl-labda- 8(9),13E-diene was easily transformed into (+)-subersic acid by demethylation of the phenol ether and ester. This cross-coupling strategy showed a good functional group tolerance and various (+)-subersic acid derivatives were obtained in moderate yields.
Heterocyclic modulators of cannabinoid receptors
-
Page/Page column 32-33; 34-35, (2016/06/06)
Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are a
An efficient synthesis of (+)-subersic acid
Wang, Jing,Wang, Peiqiang,Li, Jue,Wu, Peiying,Ren, Jiangmeng,Zeng, Bubing
, p. 679 - 682 (2015/06/25)
This paper describes a concise and practical route to (+)-subersic acid from naturally occurring (-)-Sclareol in 7 steps. The key step of this route relied on the cross coupling of the diterpene with the arene fragment using the arylation of allylic acetate followed by β-acetoxy elimination type Heck reaction. A seven-step synthetic route was developed to synthesize (+)-subersic acid from (-)-Sclareol. The cross coupling of the diterpene with the arene fragment using the arylation of allylic acetate followed by β-acetoxy elimination type Heck reaction was acted as the key reaction.
NEUROPROTECTIVE CB2 RECEPTOR AGONISTS
-
Page/Page column 0075; 0076, (2014/02/15)
A method of treating or preventing a neuroinflammatory and/or neurodegenerative disease in a subject by administering a pharmaceutically effective amount of a CB2 receptor agonist is described. The CB2 receptor agonist can be a compo
PROCESS FOR PRODUCTION OF PHENOL DERIVATIVES SUBSTITUTED WITH IODINE AT ORTHO POSITION
-
Page/Page column 6, (2010/07/06)
A process in which a phenol derivative is iodinated to produce a 2-iodophenol or 2,6-diiodophenol derivative substituted with iodine at an ortho position thereof is provided, which does not require any step of recovery of iodine but can produce it at low cost, in high yield and with high quality. A phenol derivative is mixed with a pyridine and hydrogen peroxide or iodic acid as an oxidizing agent, and reacted with molecular iodine. As a result, iodination can be performed very efficiently with iodine in an amount close to the theoretical amount relative to the phenol derivative, and the 2-iodophenol or 2,6-diiodophenol derivative can be obtained in high yield and with high quality.
A mild and simple iodination of phenols with trichloroisocyanuric acid/I2/wet SiO2 system
Akhlaghinia, Batool,Rahmani, Marzieh
experimental part, p. 3 - 6 (2010/08/19)
Molecular iodine in the presence of trichloroisocyanuric acid and wet sio2 has been utilized efficiently for iodination of phenols under mild reaction conditions.
S1P RECEPTORS MODULATORS
-
Page/Page column 107; 108, (2010/04/30)
The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.