52605-96-6Relevant articles and documents
A halogenated nitrogen-containing unsaturated cyclic hydrocarbon preparation method
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Paragraph 0018, (2018/05/16)
The invention discloses a halogenated nitrogen-containing unsaturated cyclic hydrocarbon of the preparation method, the steps of: (1) the nitrogen-containing unsaturated cyclic hydrocarbon dissolved in hydrochloric acid or hydrobromic acid, addition of an oxidizing agent, the reaction system halogenated reaction, in the reaction process timing sampling detection, when detecting the target product quality of a halide accounted for is a reaction system in the total of the organic matter of 70% - 95% when, added to the reaction system in the terminator to terminate reaction, to obtain containing nitrogen-containing unsaturated cyclic hydrocarbon feed; (2) to the liquid mixed into the organic solvent extraction, extraction to obtain the organic phase, the organic phase temperature is reduced to make the solid precipitation or distilling the organic solvent to obtain a liquid product to be deducted, the resulting solid or liquid product is halogenated nitrogen-containing unsaturated cyclic hydrocarbon. The method solves the problem of the nitrogen-containing unsaturated cyclic hydrocarbon over [...] reaction problems.
Synthetic method of 2,5,6-trimethoxy-3-picolinic acid
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Paragraph 0008, (2017/11/04)
The invention relates to a synthetic method of 2,5,6-trimethoxy-3-picolinic acid, which mainly solves the technical problem that no effective synthetic methods are provided at present. The synthetic method provided by the invention comprises the following steps: converting 2-chloro-3-hydroxypyridine hydroxy into methoxy; carrying out methoxy nucleophilic substitution of chlorine; carrying out bromination of a pyridine ring; and carrying out methoxy selective substitution of bromine; removing bromine from n-butyllithium, reacting with carbon dioxide, and introducing carboxy so as to obtain 2,5,6-trimethoxy-3-picolinic acid. In the whole synthetic process, intermediates and object products do not need to be separated through a chromatographic column, the raw materials are cheap, and the purification is simple.
PYRROLIDINE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 63; 64, (2016/07/05)
The present invention is directed to pyrrolidine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITOR
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Paragraph 0120, (2015/12/19)
Disclosed are a 2-aminopyridine derivative having protein kinase inhibition activity, a preparation method and a pharmaceutical composition thereof Also disclosed are uses of the compounds and the pharmaceutical compositions thereof in the preparation of drugs for treating and/or preventing protein kinase-related diseases.
FSH RECEPTOR ANTAGONISTS
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Page/Page column 89; 90, (2013/04/10)
The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders
Room-temperature Suzuki-Miyaura coupling of heteroaryl chlorides and tosylates
Yang, Junfeng,Liu, Sijia,Zheng, Jian-Feng,Zhou, Jianrong
supporting information, p. 6248 - 6259,12 (2020/09/16)
Suzuki-Miyaura coupling of heteroaryls is an important method for the preparation of compound libraries for medicinal chemistry and materials research. Although many catalysts have been developed, none of them have been generally applicable to the coupling reactions of heteroaryl chlorides and tosylates at room temperature. We discovered that a catalyst combination of Pd(OAc)2 and XPhos (2-dicyclohexylphosphanyl-2',4',6'- triisopropylbiphenyl) could efficiently catalyze these couplings. Besides the choice of catalyst, the use of hydroxide bases in an aqueous alcoholic solvent was essential for fast couplings. These conditions promoted fast release of active catalyst (XPhos)Pd0, and accelerated the transmetalation in the catalytic cycle. Most of the major families of heteroaryl chlorides (31 examples) and tosylates (17 examples) reached full conversion within minutes to hours at room temperature. The method could be easily scaled up for gram-scale synthesis. Furthermore, we examined the relative reactivity of coupling partners in whole reactions. Electron-rich heteroaryl chlorides and tosylates reacted more slowly than electron-deficient ones, in the order of indole, pyrrole furan, thiophene > pyridine. Similarly, electron-deficient arylboronic acids were less reactive than electron-neutral and electron-rich ones. The reactivity trends from this study can help to choose appropriate coupling partners for Suzuki reactions.
PHARMACEUTICAL COMPOUNDS
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Page/Page column 107, (2011/04/19)
The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
Camptothecin-analog with a novel, "flipped" lactone-stable, E-ring and methods for making and using same
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Page/Page column 18-19, (2008/12/04)
The present invention discloses: (i) a novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (ii) methods of synthesis of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (iii) pharmaceutically-acceptable formulations comprising said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents; (iv) methods of administration of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof; and (v) devices for the administration of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more chemotherapeutic agents, to subjects in need thereof.
CAMPTOTHECIN-ANALOG WITH A NOVEL, “FLIPPED” LACTONE-STABLE, E-RING AND METHODS FOR MAKING AND USING SAME
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Page/Page column 40, (2008/06/13)
The present invention discloses: (i) a novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (ii) methods of synthesis of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (iii) pharmaceutically-acceptable formulations comprising said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents; (iv) methods of administration of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof; and (v) devices for the administration of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more chemotherapeutic agents, to subjects in need thereof.
Antitumor agents 222. Synthesis and anti-androgen activity of new diarylheptanoids
Ohtsu, Hironori,Itokawa, Hideji,Xiao, Zhiyan,Su, Ching-Yuan,Shih, Charles C.-Y.,Chiang, Tzuying,Chang, Eugene,Lee, YiFen,Chiu, Shang-Yi,Chang, Chawnshang,Lee, Kuo-Hsiung
, p. 5083 - 5090 (2007/10/03)
Fifteen new diarylheptanoids were synthesized and evaluated for antagonistic activity against androgen receptor (AR)-mediated reporter gene transcription using DU145, PC-3, and LNCaP prostate cancer cell lines. Most compounds showed activity in a 5α-dihydrotestosterone (DHT)-induced reporter gene expression assay in DU145 cells transfected with wild-type AR. Ten compounds (5, 8, 10, 14-15, and 18-22) were equipotent with hydroxyflutamide (HF), the anti-androgen currently available for the treatment of prostate cancer. However, except for compounds 5 and 10, none of the tested compounds was significantly effective in attenuating DHT-induced reporter gene expression in LNCaP cells, which contain endogenous mutant AR.
