专利号:US-2024294462-A1 优先权日:2023-02-15 标题:Method for the Synthesis of Ionizable Lipids Using a Doubly Alkylated Intermediate 发明人:SAADATI FARIBA; TRAN HUY; CIUFOLINI MARCO; ATMURI N D PRASAD 权利人:NANOVATION THERAPEUTICS INC 摘要:Provided herein is a method for the preparation of ionizable, cationic amino lipids using a doubly alkylated nucleophilic intermediate to produce a ketone. The ketone, or a corresponding alcohol, is subjected to one or more synthesis steps to add an ionizable moiety thereto. The method can be advantageously employed for the synthesis of unsymmetrical analogues of the above lipids that would be considerably more difficult to make by alternative strategies. The method can also be used to prepare symmetrical ionizable, cationic amino lipids with fewer steps and/or with the use of fewer hazardous chemicals than known synthesis methods.
专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:WO-2012047907-A9 优先权日:2010-10-04 标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto 发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.
专利号:WO-2024105700-A1 优先权日:2022-11-18 标 题:A method for the synthesis of anthranilic amide compounds and intermediates thereof 发明人:MALVIYA NITIN; MAL SANJIB; KLAUSENER ALEXANDER G M 权利人:PI INDUSTRIES LTD 摘要:The present invention discloses a method for the synthesis of a compound of formula (V) or a salt thereof, wherein, R, R1, R2, R3, R4a and R4b are as defined in the detailed description. The method further comprises the synthesis of an anthranilic diamide compound of formula (Z).
专利号:WO-9532946-A1 优先权日:1994-05-27 标题 :Methods for the synthesis of 9-cis retinoids and their novel intermediates 发明人:BENNANI YOUSSEF L 权利人:LIGAND PHARM INC 摘要:Methods for the synthesis of 9-cis retinoids, novel intermediates and methods for the synthesis of cyclohexadienyne nitriles and 9-cis alkyl cisoid nitriles, as well as 9-cis retinoids made using such methods are provided.
专利号:WO-2025134140-A1 优先权日:2023-12-19 标题:A method for the synthesis of substituted anthranilic amide compounds, intermediates and salts thereof 发明人:MALVIYA NITIN JAIKANT; SINGH VIPENDER; SHAH JIGARKUMAR HARKISHANDAS; KALE MANOJ GANPAT; KAVITAKE SANTOSH GIRIDHAR; BORHADE AJIT SAHEBRAO; KLAUSENER ALEXANDER G M 权利人:PI INDUSTRIES LTD 摘要:The present invention discloses a method for the synthesis of compounds of formula (I) or a salt thereof, wherein, R is selected from hydrogen, halogen, cyano, C1-C12 alkyl, C1-C12 haloalkyl, C1-C12 alkoxy, C1-C12 haloalkoxy, or C3-C8 cycloalkyl; R4 is selected from hydrogen, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C1-C12 haloalkyl, C2-C12 haloalkenyl, C2-C12 haloalkynyl, C1-C12 alkoxy, C1-C12 haloalkoxy, C3-C8 cycloalkyl, or C3-C8 cycloalkyl-C1-C10 alkyl; and n represents an integer selected from 0-4. The method further comprises the synthesis of an anthranilic diamide compound of formula (A).
[参考文献]: F Giallongo, Et Al. Effects Of Slow-Release Urea And Rumen-Protected Methionine And Histidine On Performance Of Dairy Cows. J Dairy Sci. 2015 May;98(5):3292-308.
合成参考文献
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