专利号:US-5512701-A 优先权日:1995-06-07 标题:Process for the synthesis of vinyl sulfenic acid derivatives 发明人:HOARD DAVID W; LUKE WAYNE D 权利人:LILLY CO ELI 摘要:The present invention is directed to a new process for the synthesis of vinyl sulfenic acid derivatives. These compounds are useful for the synthesis of benzo[b]thiophenes, in particular 2-aryl-benzo[b]thiophenes.
专利号:WO-2022155981-A1 优先权日:2021-01-25 标题 :USE OF N-HETEROCYCLIC CARBENE-BASED COMPOUNDED NICKEL (II) COMPLEX IN SYNTHESIS OF α-BENZYL BENZOFURAN COMPOUND 发明人:SUN HONGMEI; SHUI YU; JIN WENHUI 权利人:UNIV SOOCHOW 摘要:Disclosed is the use of an N-heterocyclic carbene-based compounded nickel (II) complex in the synthesis of an α-benzyl benzofuran compound. In the present invention, an air-stable compounded nickel (II) complex Ni[P(OEt) 3 ]{[R`NC(CH 3 )C(CH 3 )NR`]C}Br 2 is used as a catalyst, wherein R` is 2,4,6-trimethylphenyl, and the α-benzyl benzofuran compound is synthesized by means of a hydrogen heteroarylation reaction of an aryl ethylene compound and a benzofuran compound in the presence of an organic base. The operability and substrate applicability of the catalyst are obviously better than those of the prior art, and meanwhile, the nickel catalyst has a higher practical application value due to the air stability and easiness of synthesis thereof.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 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 substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-6998484-B2 优先权日:2000-10-04 标 题:Synthesis of purine locked nucleic acid analogues 发明人:KOCH TROELS; JENSEN FLEMMING REISSIG 权利人:SANTARIS PHARMA AS 摘要:The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic substitution reaction of the 6-substituent in the purine ring and simultaneous nucleophile-induced intramolecular ring closure of the C-branched carbohydrate to form novel purine LNA analogues. The novel strategy is illustrated by the synthesis of the novel compound (1S,3R,4R,7S)-7-benzyloxy-1-methanesulfonylmethyl-3-(guanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane which is easily converted into (1S,3R,4R,7S)-7-hydroxy-1-hydroxymethyl-3-((2-N-isobutyrylguanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane after isobutyryl protection of the 2-amino purine group and subsequent substitution of 1-methanesulfonyl with benzoate, debenzoylation and debenzylation.
专利号:US-2023174567-A1 优先权日:2020-05-22 标题:Synthesis of fluorinated nucleotides 发明人:ARMIGER TRAVIS; BELYK KEVIN M; BENKOVICS TAMAS; CHUNG CHEOL K; JI CHEN YINING; JOHNSON HEATHER CLAIRE; KLAPARS ARTIS; LIU ZHIJIAN; LIU ZHUQING; MOORE JEFFREY C; NEEL ANDREW J; PENG FENG; RUMMELT STEPHAN M; SALEHI MARZUARANI NASTARAN; SHERRY BENJAMIN D; SONG ZHIGUO JAKE; TURNBULL BEN WILLIAM HULME; WANG LU; XU FENG 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (2S,3R,4S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-fluoro-4-hydroxy-2-(mercaptomethyl)tetrahydrofuran-3-yl dihydrogen phosphate, also known as 3′-fluoro-thio-guanosine monophosphate or 3′-F-thio-GMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation. (I)
摘要:Abell, A. D.; Edmonds, M. K., Science of Synthesis, (2009) 46, 44. 摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 147. 摘要:Kobayashi, J.; Kawashima, T., Science of Synthesis Knowledge Updates, (2014) 1, 356. 摘要:Kobayashi, J.; Kawashima, T., Science of Synthesis Knowledge Updates, (2014) 1, 366. 摘要:Naka, H.; Saito, S., Science of Synthesis Knowledge Updates, (2010) 4, 72.