专利号:US-8513465-B2 优先权日:2008-02-04 标题:Potassium organotrifluoroborate derivative and a production method therefor 发明人:KANG HEONJOONG; HAM JUNGYEOB; AHN HONG RYUL; PARK YOUNG HEE 权利人:KANG HEONJOONG; HAM JUNGYEOB; AHN HONG RYUL; PARK YOUNG HEE; SNU R&DB FOUNDATION 摘要:Provided are a production method for a potassium organotrifluoroborate compound having a hydroxyl group, and a novel potassium organotrifluoroborate compound having a hydroxyl group. The production method is advantageous in that a potassium organotrifluoroborate compound can be produced in a single reaction without recourse to a process of isolating and purifying an intermediate. The novel potassium organotrifluoroborate compound having a hydroxyl group is useful as a reactant which is widely used in the total synthesis of physiologically active natural products and diverse organic synthesis reactions including halogen substitution reactions, 1,2- and 1,4-addition reactions using a rhodium (Rh) catalyst, and Suzuki coupling reactions using a palladium (Pd) catalyst.
专利号:US-5116987-A 优先权日:1988-12-26 标题:Method of preparing chroman derivatives, and synthesis intermediates 发明人:GARCIA GEORGES; METTEFEU DANIEL; ROUX RICHARD 权利人:SANOFI SA 摘要:The invention describes a method of synthesizing a compound of the formula ##STR1## in which X=O or NR, n Z=an electron-attracting group, n R=H, CN or NO 2 , n R 1 +R 2 +N--Câ•?X=a 5-membered or 6-membered heterocycle, and n R 3 =H, R 4 =OH or R 3 +R 4 =a bond, n said method involving intermediates of the formula ##STR2## in which R 5 =H, Br or N(R 1 )CXR 2 . This method of synthesis does not involve the epoxide derivative of the chroman. n The novel compounds of formula (IX) form a further subject of the invention.
专利号:US-9994558-B2 优先权日:2013-09-20 标题 :Multicyclic compounds and methods of using same 发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).
专利号:US-9505799-B2 优先权日:2011-05-13 标题:18F-labeled precursor of PET radioactive medical supplies, and preparation method thereof 发明人:CHI DAE-YOON; LEE BYOUNG-SE; PARK CHANSOO; LEE MIN-HYUNG; CHA HYOJIN; CHO WOOJIN; KANG HEEWON; KIM KYUNGHUN 权利人:CHI DAE-YOON; LEE BYOUNG-SE; PARK CHANSOO; LEE MIN-HYUNG; CHA HYOJIN; CHO WOOJIN; KANG HEEWON; KIM KYUNGHUN; FUTURECHEM CO LTD 摘要:The present invention relates to a precursor of positron emission tomography (PET) radioactive medical supplies, a preparation method thereof, and an application thereof, and more specifically, to a precursor having a tetravalent organic salt leaving group, a preparation method, and a method for preparing desired PET radioactive medical supplies in a high radiochemical yield within a short preparation time by introducing 18 F using the same through a single step. The precursor having a tetravalent organic salt leaving group of the present invention can simplify the known complex multistep preparation of radioactive medical supplies into a single step, can save production costs because an excessive amount of a phase transfer catalyst is not required, facilitates separation of a compound after reaction, and enables rapid reaction velocity. The features are appropriate for the mass production of PET radioactive medical supplies by an automated synthesis system.
专利号:US-9938258-B2 优先权日:2012-11-29 标 题:Substituted 2,3-dihydrobenzofuranyl compounds and uses thereof 发明人:BALOGLU ERKAN; SHECHTER SHARON; SHACHAM SHARON; MCCAULEY DILARA; SENAPEDIS WILLIAM; GOLAN GALI; KALID ORI 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to substituted 2,3-dihydrobenzofuranyl compounds, and more particularly to a compound represented by Structural Formula I: n nor a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.
专利号:CN-113797212-B 优先权日:2020-06-11 标 题:Synthesis method and activity study of a group of antibacterial drugs containing mannose structure