专利号:US-9862745-B2 优先权日:2004-03-30 标题 :Synthesis of boronic ester and acid compounds 发明人:AMMOSCATO VINCE; BISHOP JOHN E; CHIU FANG-TING; GEISER ACHIM; GOMEZ JEAN-MARC; HETT ROBERT; KOELLNER CHRISTOPH; KULKARNI VITHALANAND R; LO YOUNG; MUNK STEPHEN; PICKERSGILL I FRASER 权利人:MILLENNIUM PHARM INC; MILLENNIUM PHARM INC 摘要:The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.
专利号:US-9243004-B2 优先权日:2011-07-22 标题 :Synthesis of boronic esters and boronic acids using grignard reagents 发明人:CLARY JACOB W; SINGARAM BAKTHAN 权利人:CLARY JACOB W; SINGARAM BAKTHAN; UNIV CALIFORNIA 摘要:Boronic esters and boronic acids are synthesized at ambient temperature in an ethereal solvent by the reaction of Grignard reagents with a boron-containing substrate. The boron-containing substrate may be a boronic ester such as pinacolborane, neopentylglycolborane, or a dialkylaminoborane compound such as diisopropylaminoborane. The Grignard reagents may be pre-formed or generated from an alkyl, alkenyl, aryl, arylalkyl, heteroaryl, vinyl, or allyl halide compound and Mg 0 . When the boron-containing substrate is a boronic ester, the reactions generally proceed at room temperature without added base in about 1 to 3 hours to form a boronic ester compound. When the boron-containing substrate is a dialkylaminoborane compound, the reactions generally proceed to completion at 0° C. in about 1 hour to form a boronic acid compound.
专利号:US-8207337-B2 优先权日:2007-01-29 标 题:Reagent for organic synthesis reaction containing organic triol borate salt 发明人:MIYAURA NORIO; YAMAMOTO YASUNORI 权利人:MIYAURA NORIO; YAMAMOTO YASUNORI; WAKO PURE CHEM IND LTD 摘要:[Problem] n To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. n [Means for Solving Problems] n The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R 1 represents alkyl, alkenyl, etc.; R 2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m + represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M 2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).
专利号:US-2018265546-A1 优先权日:2004-03-30 标题 :Synthesis of boronic ester and acid compounds
专利号:US-2005240047-A1 优先权日:2004-03-30 标 题:Synthesis of boronic ester and acid compounds
专利号:US-2020157143-A1 优先权日:2004-03-30 标题 :Synthesis of boronic ester and acid compounds
摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 63. 摘要:Hall, D. G.; Zheng, H., Science of Synthesis Knowledge Updates, (2011) 4, 100. 摘要:Yi, C. S., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 242.