2698-69-3Relevant articles and documents
O-(DIHYDROBENZOFURANYL)-DIBENZO-α-PYRONES FROM UMTIZA LISTERANA
Burger, Adrian P. N.,Brandt, Edward V.,Roux, David G.
, p. 2813 - 2818 (1983)
The novel metabolites (2'S,3'R)-3,10-dihydroxy-9-O-(6'-hydroxy-2'-hydroxymethyldihydrofuran-3-yl)-dibenz--pyran-6-one and its 5',6'-dihydroxy analogue are accompanied in the heartwood of Umtiza listerana by several known flavonoids and the parent 3,9,10-trihydroxydibenz--pyran-6-one.The latter, used for structural elucidation of the complex dibenzo-α-pyrones, was synthesized via a Hurtley condensation.Key Word Index-Umtiza listerana; Leguminosae; heartwood metabolites; (2'S,3'R)-3,10-dihydroxy-9-O-(6'-hydroxy-2'-hydroxymethyldihydrobenzofuran-3-yl)-dibenz--pyran-6-one; (2'S,3'R)-3,10-dihydroxy-9-O-(5',6'-dihydroxy-2'-hydroxymethyldihydrobenzofuran-3-yl)-dibenz--pyran-6-one; 3,9,10-trihydroxydibenz--pyran-6-one; flavonoids; 1H NMR; synthesis.
Preparation method of 3-hydroxy-4-methoxy-2-nitrobenzoic acid
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Paragraph 0050-0052; 0057-0059; 0064-0066, (2020/07/12)
The invention discloses a preparation method of 3-hydroxy-4-methoxy-2-nitrobenzoic acid, and belongs to the field of synthesis of medical intermediates. The preparation method comprises the followingsteps: starting from 3-alkoxy-4-acetoxybenzaldehyde (1), carrying out a nitration reaction process to obtain an intermediate (2), removing acetyl from the intermediate (2) to obtain an intermediate (3), methylating to obtain an intermediate (4), oxidizing the intermediate (4) to obtain an intermediate (5), deprotecting the intermediate (5), and recrystallizing to remove the isomer, thereby obtaining the 3-hydroxy-4-methoxy-2-nitrobenzoic acid (6). The method is simple, convenient and stable to operate, high in yield, environment-friendly, low in production cost and suitable for industrial large-scale production, and products in all steps are easy to separate.
BORON-CONTAINING SMALL MOLECULES
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Paragraph 0295, (2017/09/19)
Compounds, pharmaceutical formulations, and methods of treating bacterial infections are disclosed.
Class of large ring heterocyclic compound restraining HCV and manufacturing and uses thereof
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Paragraph 0309; 0310; 0312, (2017/09/01)
The invention relates to a class of compounds that inhibit HCV. The compounds are represented by Formula A. The invention also relates to preparation and pharmaceutical use of the compounds.
METHOD FOR PREPARING DIPHENYLMETHANE DERIVATIVES
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Paragraph 0197; 0198; 0199; 0200, (2017/09/29)
The present invention relates to an improved process for preparing a diphenyl methane derivative which is useful as an inhibitor of a sodium-dependent glucose transporter (SGLT). Since the process of the present invention is performed by convergent synthe
Design, synthesis and biological evaluation of 2,3-dihydroimidazo[1,2-: C] quinazoline derivatives as novel phosphatidylinositol 3-kinase and histone deacetylase dual inhibitors
Wu, Yichao,Dai, Weichen,Chen, Xin,Geng, Aixin,Chen, Yadong,Lu, Tao,Zhu, Yong
, p. 52180 - 52186 (2017/11/22)
Histone deacetylase (HDAC) inhibitors are known to induce multiple epigenetic modifications affecting signaling networks and act synergistically with phosphatidylinositol 3-kinase (PI3K) inhibitors for the treatment of cancer. Herein we present a novel design approach for cancer drug development by incorporating HDAC inhibitory functionality into a PI3K inhibitor pharmacophore to construct dual-acting inhibitors. The designed compounds were synthesized and showed inhibitory activities against PI3K and HDAC. The representative dual PI3K/HDAC inhibitors, compounds 12a-j, showed potent antiproliferative activities against K562 and Hut78 in cellular assays. This work may lay the foundation for developing novel dual PI3K/HDAC inhibitors as potential anticancer therapeutics.
SYNTHESIS OF PI3K INHIBITOR AND SALTS THEREOF
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Page/Page column 40-41, (2016/06/01)
The present invention relates to a novel method of preparing a compound of formula (I) or salt thereof, to novel intermediate compounds, to the use of said novel intermediate compounds for the preparation of said compound of formula (I) or salt thereof. T
Discovery and SAR of Novel 2,3-Dihydroimidazo[1,2-c]quinazoline PI3K Inhibitors: Identification of Copanlisib (BAY 80-6946)
Scott, William J.,Hentemann, Martin F.,Rowley, R. Bruce,Bull, Cathy O.,Jenkins, Susan,Bullion, Ann M.,Johnson, Jeffrey,Redman, Anikó,Robbins, Arthur H.,Esler, William,Fracasso, R. Paul,Garrison, Timothy,Hamilton, Mark,Michels, Martin,Wood, Jill E.,Wilkie, Dean P.,Xiao, Hong,Levy, Joan,Stasik, Enrico,Liu, Ningshu,Schaefer, Martina,Brands, Michael,Lefranc, Julien
, p. 1517 - 1530 (2016/08/27)
The phosphoinositide 3-kinase (PI3K) pathway is aberrantly activated in many disease states, including tumor cells, either by growth factor receptor tyrosine kinases or by the genetic mutation and amplification of key pathway components. A variety of PI3K isoforms play differential roles in cancers. As such, the development of PI3K inhibitors from novel compound classes should lead to differential pharmacological and pharmacokinetic profiles and allow exploration in various indications, combinations, and dosing regimens. A screening effort aimed at the identification of PI3Kγ inhibitors for the treatment of inflammatory diseases led to the discovery of the novel 2,3-dihydroimidazo[1,2-c]quinazoline class of PI3K inhibitors. A subsequent lead optimization program targeting cancer therapy focused on inhibition of PI3Kα and PI3Kβ. Herein, initial structure–activity relationship findings for this class and the optimization that led to the identification of copanlisib (BAY 80-6946) as a clinical candidate for the treatment of solid and hematological tumors are described.
SYNTHESIS OF COPANLISIB AND ITS DIHYDROCHLORIDE SALT
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Page/Page column 47, (2016/06/01)
The present invention relates to a novel method of preparing copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride. The present invention also relates to copanlisib dihydrochloride hydrates as compounds.
SYNTHESIS OF PI3K INHIBITOR AND SALTS THEREOF
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Page/Page column 42, (2016/06/01)
The present invention relates to a novel method of preparing a compound of formula (I) or salt thereof, to novel intermediate compounds, to the use of said novel intermediate compounds for the preparation of said compound of formula (I) or salt thereof an