专利号:US-7205427-B2 优先权日:2002-06-04 标 题:Cross-coupling synthesis of alkyl (dialkylphenyl) indenes 发明人:BARNES HAMLIN H 权利人:BOULDER SCIENT CO 摘要:A cross-coupling synthesis of 2-alkyl-4-(2,6-dialkylphenyl)indenes is described. A 2-alkylidene is treated with a dialkylboronic acid in the presence of a catalyst. A feature of the invention is the use of a cross-coupling catalyst comprising palladium dichloride (1,5-cyclooctadiene) as a cross-coupling catalyst.
专利号:US-7632975-B2 优先权日:2004-12-22 标 题:Process for the synthesis of arylfluorenes and analogs thereof 发明人:HEIDENHAIN SOPHIE 权利人:CDT OXFORD LTD 摘要:A process is provided for the synthesis of a compound of formula (I): n nwherein:n M=0 or 1; N and p are 0 or 1 to 4; X is a single bond, O, S or NH; And R 1 -R 4 are as defined in claim 1.
专利号:US-6958420-B2 优先权日:2002-07-19 标题:Synthesis of aminoarylboronic esters and substituted anilines from arenes via catalytic C-H activation/borylation/amination and uses thereof 发明人:MALECZKA JR ROBERT E; SMITH III MILTON R; HOLMES DANIEL 权利人:UNIV MICHIGAN STATE 摘要:A process is described for synthesizing aminoarylboronic esters of the general formula n n nwherein R, R 2 , and R 3 are each an alkyl, aryl, vinyl, alkoxy, carboxylic esters, amides, or halogen; Ar is any variety of phenyl, naphthyl, anthracyl, heteroaryl; and R 1 is alkyl, hydrogen, or aryl. The aminoarylboronic esters are produced via the metal-catalyzed coupling of arylboronic esters of the general formula n n nwherein R and R 1 are any non-interfering group and X is chloro, bromo, iodo, triflates, or nonaflates to amines (primary and secondary). In particular, a process is described for the synthesis of the aminoarylboronic esters via a step-wise or tandem process in which one catalytic event is a metal-catalyzed borylation and the other catalytic event is a metal-catalyzed amination.
专利号:US-2024336649-A1 优先权日:2021-06-21 标 题 :Synthesis of covalent protein dimers that can inhibit myc-driven transcription 发明人:LOAS ANDREI; PENTELUTE BRADLEY L; POMPLUN SEBASTIAN; JBARA MUHAMMAD; SCHISSEL CARLY KATHERINE; RODRIQUEZ JACOB JOSHUA LEE; BUCHWALD STEPHEN LEFFLER; BOIJA ANN; KLEIN ISAAC; HAWKEN SUSANA WILSON; LI CHARLES HAN 权利人:MASSACHUSETTS INST TECHNOLOGY; WHITEHEAD INSTITUTE OF BIOMEDICAL RES 摘要:The disclosure relates to covalent protein dimers of MYC, MAX, and Omomyc; pharmaceutical compositions comprising the covalent protein dimers; methods of making the covalent protein dimers; and methods of treating disorders associated with MYC dysregulation (e.g., cancer) with the covalent protein dimers.
专利号:US-12049470-B2 优先权日:2021-02-01 标 题 :MK2 inhibitors, the synthesis thereof, and intermediates thereto 发明人:RUCHELMAN ALEXANDER L; COOMBS JOHN R; ZHU KEMING; LIM DANIEL; JOE CANDICE LEE; GEORGE DAVID T; ZHENG BIN; LIN DONG 权利人:CELGENE CORP 摘要:The present disclosure provides novel synthetic intermediates useful in the synthesis of MK2 kinase inhibitors.
专利号:US-11718584-B2 优先权日:2019-02-22 标题 :Process for the synthesis anthranilic diamide compounds and intermediates thereof 发明人:KARRI PHANEENDRASAI; PABBA JAGADISH; SHINDE BHARAT UTTAMRAO; KALWAGHE AMOL DNYANESHWAR; MADHAVRAO KAMBLE MARUTI; KLAUSENER ALEXANDER G M; PANMAND DEEPAK SHANKAR 权利人:PI INDUSTRIES LTD 摘要:The present invention disclosed a process for the synthesis of anthranilic diamide compound of formula (I), n n n n n n n n n n wherein, R 1 , R 2 , R 3a , R 3b , R 3c , R 4 , R 5 , R 6 and Z are as defined in the detailed description. The process comprising the step of obtaining a mono- or dicyano substituted aniline compound of formula (IV) which is then converted to an anthranilic acid compound of formula (V) or an anthranilic amide compound of formula (Va). Further, the compound of formula (VI) can be optionally synthesized from compound of formula (IV or V or Va)
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