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-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-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)
专利号:US-2023150994-A1 优先权日:2020-04-07 标 题:Methods for synthesis of chk1 inhibitors 发明人:SCHWAEBE MICHAEL; ROSNER THORSTEN; ZHAO DALIAN; MILLER ROSS; DULINA RICH; HUMORA MICHAEL; GOTTSCHLING STEPHEN E 权利人:SIERRA ONCOLOGY INC 摘要:The present technology relates to processes, compounds, compositions, and methods useful for coupling reactions. Also, the present disclosure provides for novel intermediates, compositions of matter, and processes relating to the Chk1 inhibitor, SRA737.
专利号:US-2004024237-A1 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