cas 30951-66-7, 2-(3-Bromophenyl)propan-2-ol

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Stoldt,Turk
p. 2370
(1969)
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Stepwise benzylic oxygenation via uranyl-photocatalysis
Stepwise oxygenation at the benzylic position (1°, 2°, 3°) of aromatic molecules was comprehensively established under ambient conditions via uranyl photocatalysis to produce carboxylic acids, ketones, and alcohols, respectively. The accuracy of the stepwise oxygenation was ensured by the tunability of catalytic activity in uranyl photocatalysis, which was adjusted by solvents and additives demonstrated through Stern–Volmer analysis. Hydrogen atom transfer between the benzylic position and the uranyl catalyst facilitated oxygenation, further confirmed by kinetic studies. Considerably improved efficiency of flow operation demonstrated the potential for industrial synthetic application.
Hu, Deqing,Jiang, Xuefeng
supporting information
p. 124 - 129
(2022/01/19)

Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes
According to the binding mode of ABBV-744 with bromodomains and the cape space of HDAC, the novel selective HDAC/BRD4 dual inhibitors were designed and synthesized by the pharmacophore fusion strategy. Evaluating the biomolecular activities through SARs exploration identified three kinds of selective dual inhibitors 41c (HDAC1/BRD4), 43a (pan-HDAC/BRD4) and 43d (HDAC6/BRD4(BD2)), whose target-related cellular activities in MV-4-11 cells were also confirmed. Significantly, the selective dual inhibitor 41c (HDAC1/BRD4) exhibited synergistic effects against MV-4-11 cells, which strongly induced G0/G1 cell cycle arrest and apoptosis, and the first HDAC6/BRD4(BD2) dual inhibitor was found. This study provides support for selective HDAC/BRD4 dual inhibitors as epigenetic probes based on pyrrolopyridone core for the future biological evaluation in different cancer cell lines.
Chen, Jingjing,Li, Yalei,Zhang, Jie,Zhang, Minmin,Wei, Aihuan,Liu, Hongchun,Xie, Zhicheng,Ren, Wenming,Duan, Wenwen,Zhang, Zhuo,Shen, Aijun,Hu, Youhong
supporting information

(2020/10/20)

Pyrrolopyridone compound as well as preparation method, composition and application thereof
The invention relates to a pyrrolopyridone compound or pharmaceutically acceptable salts thereof, and a preparation method and application thereof. The pyrrolopyridone compound has a structure as shown in a formula I which is described in the specification. The compound has the characteristic of BRD4 and HDAC double-target inhibition activity and/or has the characteristic of a function of targetedubiquitination degradation of BRD4 protein, and can be applied to related diseases such as tumor resistance related to the target.
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Paragraph 0332; 0337-0339

(2020/12/30)

Synthesis of 4H-1,3-Benzoxazines via Metal- and Oxidizing Reagent-Free Aromatic C-H Oxygenation
An unprecedented electrochemical aromatic C-H oxygenation reaction for the synthesis of 4H-1,3-benzoxazines from easily available N-benzylamides is reported. These oxidative cyclization reactions proceed in a transition metal- and oxidizing reagent-free fashion and produce H2 as only theoretical byproduct. Adapting the C-H oxygenation reaction in an electrochemical microreactor has been demonstrated.
Xu, Fan,Qian, Xiang-Yang,Li, Yan-Jie,Xu, Hai-Chao
supporting information
p. 6332 - 6335
(2017/12/08)

GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy.
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Page/Page column 122

(2015/06/25)

Glucosylceramide synthase inhibitors
The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
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Page/Page column 50

(2015/09/28)

1,3,5-TRIAZINE-2-AMINE DERIVATIVES, PREPARATION THEREOF AND DIAGNOSTIC AND THERAPEUTIC USE THEREOF
The present invention relates to compounds corresponding to formula (I) in which: - R1 represents a substituted phenyl; - R2 represents: - a substituted phenyl; - a heteroaromatic group, the said group being unsubstituted or substituted one or more times; - R3 represents a group Alk; - R4 represents a hydrogen atom or a (C1-C4)alkyl; - R5 represents a hydrogen atom, a (C3-C6)cycloalkyl or a (C1-C4)alkyl-O-Alk; - or alternatively R4 and R5, together with the nitrogen atom to which they are attached, constitute a heterocyclic radical chosen from: azetidin-1-yl, pyrrolidin-1-yl, piperid-1-yl, morpholin-4-yl; - R6 represents a group -COOAlk, a group -CONH2 or a group -NHSO2 Alk; - Alk represents a (C1-C4)alkyl, which is unsubstituted or substituted one or more times with a halogen atom; in the form of the base or of an acid-addition salt. Preparation process and diagnostic and therapeutic use
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Page/Page column 15

(2013/07/05)

Access to "friedel-Crafts-Restricted" tert -alkyl aromatics by activation/methylation of tertiary benzylic alcohols
Herein we describe a two-step protocol to prepare m-tert-alkylbenzenes. The appropriate tertiary benzylic alcohols are activated with SOCl2 or concentrated HCl and then treated with trimethylaluminum, affording the desired products in 68-97% yields (22 examples). This reaction sequence is successful in the presence of a variety of functional groups, including acid-sensitive and Lewis-basic groups. In addition to t-Bu groups, 1,1-dimethylpropyl and 1-ethyl-1-methylpropyl groups can also be installed using this method.
Hartsel, Joshua A.,Craft, Derek T.,Chen, Qiao-Hong,Ma, Ming,Carlier, Paul R.
experimental part
p. 3127 - 3133
(2012/05/20)

Design, synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors
A series of gem-dimethyl-bearing C-glucosides were designed and synthesized as SGLT2 inhibitors, with anhydrous aluminum chloride-mediated Friedel-Crafts alkylation to construct the gem-dimethyl functionality being the key step. The in vivo anti-hyperglycemic activity was evaluated with mice oral glucose tolerance test (OGTT), and all the synthesized compounds showed significant but less potent anti-hyperglycemic activity than the positive control dapagliflozin.
Zhao, Wen Jing,Shi, Yong Heng,Zhao, Gui Long,Wang, Yu Li,Shao, Hua,Da Tang, Li,Wang, Jian Wu
p. 1215 - 1218
(2012/02/02)

POLYSUBSTITUTED 2-ARYL-6-PHENYLIMIDAZO[1,2-A]PYRIDINE DERIVATIVES, AND PREPARATION AND THERAPEUTIC USE THEREOF
Compounds of formula (I): wherein R, R1, R2, R3, R4, and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
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Page/Page column 8

(2011/04/18)

POLYSUBSTITUTED DERIVATIVES OF 2-HETEROARYL-6-PHENYLIMIDAZO[1,2-a]PYRIDINES, AND PREPARATION AND THERAPEUTIC USE THEREOF
Compounds of formula (I): wherein R, R1, R2, R3, R4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
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Page/Page column 15-16

(2011/04/18)

Sequential Birch reaction and asymmetric Ir-catalyzed hydrogenation as a route to chiral building blocks
A range of 1,2,4-trisubstituted cyclohexadienes obtained from the Birch reaction were hydrogenated asymmetrically to produce synthetically valuable chiral compounds in high enantio- and diastereoselectivity. The Royal Society of Chemistry.
Paptchikhine, Alexander,Itto, Kaori,Andersson, Pher G.
supporting information; experimental part
p. 3989 - 3991
(2011/06/09)

BENZOFURAN AND BENZOTHIOPHENE DERIVATIVES USEFUL IN THE TREATMENT OF CANCERS OF THE CENTRAL NERVOUS SYSTEM
The present invention relates to benzofuran and benzothiophene derivatives and compositions containing such compounds for the production of medicaments for the treatment of cancers of the central nervous system as monotherapy or combination with other agents.
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Page/Page column 50

(2008/06/13)

Comparative approaches toward diamines containing spatially separated homobenzylic and benzylic nitrogen stereocenters
Several synthetic strategies to diamines 1-3 are described. The optimum approach via opening of aziridine afforded 1-3 in 29-60% yield over 3-5 steps. A study on formation of the benzylic stereocenter using Toste's rhenium-catalyzed asymmetric reduction of phosphinyl ketimines was also evaluated and afforded 15 in 92% de.
Achmatowicz, Michal,Chan, Johann,Wheeler, Philip,Liu, Longbin,Faul, Margaret M.
p. 4825 - 4829
(2008/02/05)

Dihydropyrazolopyrimidinone derivatives
The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
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Page/Page column 42

(2008/06/13)

BENZOFURAN DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS
The invention relates to novel heterocycles of formula (I), processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.
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Page/Page column 103

(2008/06/13)

2-AMINO- AND 2-THIO-SUBSTITUTED 1,3-DIAMINOPROPANES
Disclosed are compounds of the formula: where variables Q, Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer’s disease and other diseases characterized by deposition of A beta peptide in a mammal.
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Page/Page column 189-190

(2008/06/13)

SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
The present invention relates to pyrimidinones and pyridones and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ? cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
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Page/Page column 51

(2008/06/13)

NOVEL BENZYL(IDENE)-LACTAM DERIVATIVES
The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula (I) wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13, X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.
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Page/Page column 36

(2008/06/13)

BENZOFURAN AND BENZOTHIOPHENE DERIVATIVES USEFUL IN THE TREATMENT OF HYPER-PROLIFERATIVE DISORDERS
This invention relates to novel benzofuran and benzothiophene derivatives of the general formula and their use for the treatment of hyper-proliferative disorders.
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Page/Page column 27

(2008/06/13)

Electronic Effects on Triplet and Singlet Excited-State Carbonyl Formation in the Thermolysis 3-Aryl-3-methyl-1,2-dioxetanes
A series of para- and meta-substituted 3-aryl-3-methyl-1,2-dioxetanes (1) was studied in order to evaluate the electronic effect of substituents on the efficiencies of excited-state carbonyl production.All substituents reduced the efficiency of triplet carbonyl production.Several correlations point to the formation of a triplet carbonyl exciplex, originating from a triplet biradical, in the thermolysis of 1.It also appears that substituent variation in the proacetophenone portion of 1 results in triplet efficiency changes primarily in formaldehyde, which can be rationalized in terms of a triplet exciplex.Substituent effects on singlet (S1) efficiency are markedly different from those observed with triplet efficiencies.The possibility of heavy-atom effects in 1 was pursued with p-Br and m-Br substituents.No detectable heavy-atom effect was observed with singlet (S1) efficiencies, but the p-Br substituent appeared to decrease the triplet efficiency.This suggests that a p-Br heavy-atom effect may operate from the triplet exciplex, providing the approximations used in the evaluations of the heavy-atom effect are valid.The effect of substituents on rate of thermolysis of 1 provides further evidence for a biradical mechanism.
Richardson, William H.,Stiggal-Estberg, Diana L.
p. 4173 - 4179
(2007/10/02)