专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
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-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-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-8119835-B2 优先权日:2006-12-28 标 题:Method for preparation of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphtoic acid 发明人:KALVINSH IVARS; CHERNOBROVIJS ALEKSANDRS; TRIBULOVICH VYACHESLAV; LABEISH VLADIMIR 权利人:KALVINSH IVARS; CHERNOBROVIJS ALEKSANDRS; TRIBULOVICH VYACHESLAV; LABEISH VLADIMIR; JSC GRINDEKS 摘要:A method for preparation of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid is disclosed based on “one potâ€? synthesis approach including a direct synthesis of boronic acid derivative from 2-(1-adamantyl)-4-bromoanisole and cycloboranes with a subsequent Suzuki-Miyaura coupling with 6-halonaphtenoates and basic hydrolysis of the reaction product in ethylene glycol or 1,2-propanediol.
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)