专利号:WO-2023227996-A1 优先权日:2022-05-24 标题 :A deuterated amine compounds and process for synthesis thereof 发明人:AMBATI VIJAY; KOTHARI MANISH; JONNALAGADDA NAGASIVARAO; ALETI RANJITH; KANDASAMY DR SAKHTIVEL; ROHIT CHITTALURI KRISHNA; REDDY KATUKURI MALLIKHARJUNA 权利人:CLEARSYNTH LABS LTD 摘要:The present invention relates to a process for synthesis of a deuterated compound. Most particularly, it relates to synthesis of a deuterated amine compounds of formula (l) and salts thereof. The said compound is an important key intermediate in the synthesis of deuterated drugs and/or chemical compounds.
专利号:US-9428524-B2 优先权日:2010-05-25 标 题:Synthetic process for the manufacture of ecteinascidin compounds 发明人:MARTIN LÓPEZ MA JESÚS; FRANCESCH SOLLOSO ANDRÉS; CUEVAS MARCHANTE MARIA DEL CARMEN 权利人:MARTIN LÓPEZ MA JESÚS; FRANCESCH SOLLOSO ANDRÉS; CUEVAS MARCHANTE MARIA DEL CARMEN; PHARMA MAR SA 摘要:This invention relates to compounds of formula II: wherein R 1 , R 2 , Prot SH , and Prot NH are as defined, to processes for the synthesis of ecteinascidins of formula I from compounds of formula II, and to processes for the synthesis of compounds of formula II.
专利号:US-2009012120-A1 优先权日:2006-05-10 标题:Synthesis of N-heterocycles, beta-amino acids, and allyl amines via aza-payne mediated reaction of ylides and hydroxy aziridines 发明人:BORHAN BABAK; SCHOMAKER JENNIFER M; BHATTACHARJEE SOMNATH; KORTHALS KEITH 权利人:UNIV MICHIGAN STATE 摘要:An ylide-based aza-Payne rearrangement of 2,3-aziridin- 1 -ols leads to an efficient process for the preparation of pyrrolidines. The aza-Payne rearrangement under the basic reaction conditions favors the formation of epoxy amines. Subsequent nucleophilic attack of the epoxide by the ylide yields a bis-anion, which upon a 5-exo-tet ring closure yields the desired pyrrolidine, thus completing the relay of the 3-membered the 5-membered nitrogen containing ring system. This process takes place with complete transfer of stereochemical fidelity, and can be applied to sterically hindered aziridinols.
专利号:US-8680294-B2 优先权日:2009-07-29 标题 :Enantio- and stereo specific synthesis of β-amino-α-hydroxy amides 发明人:TRAVERSE JOHN; LEONG WILLIAM M; MILLER STEVEN P; ALBANEZE-WALKER JENNIFER; HUNTER THOMAS J; WANG LIJUN; LIAO HONGBIAO; ARASAPPAN ASHOK; TRZASKA SCOTT T; SMITH RANDI M; LEKHAL AZZEDDINE; BOGEN STEPHANE L; KONG JIANSHE; BENNETT FRANK; NJOROGE F GEORGE; POIRIER MARC; KUO SHEN-CHUN; CHEN YONGGANG; MATTHEWS KENNETH S; DEMONCHAUX PATRICE; FERREIRA AMADEO 权利人:TRAVERSE JOHN; LEONG WILLIAM M; MILLER STEVEN P; ALBANEZE-WALKER JENNIFER; HUNTER THOMAS J; WANG LIJUN; LIAO HONGBIAO; ARASAPPAN ASHOK; TRZASKA SCOTT T; SMITH RANDI M; LEKHAL AZZEDDINE; BOGEN STEPHANE L; KONG JIANSHE; BENNETT FRANK; NJOROGE F GEORGE; POIRIER MARC; KUO SHEN-CHUN; CHEN YONGGANG; MATTHEWS KENNETH S; DEMONCHAUX PATRICE; FERREIRA AMADEO; MERCK SHARP & DOHME 摘要:Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.
专利号:US-8487094-B2 优先权日:2008-07-25 标题 :Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 发明人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA 权利人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA; BOEHRINGER INGELHEIM INT 摘要:Disclosed are syntheses of 11β-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).
专利号:US-6573387-B1 优先权日:1997-03-21 标 题 :Synthesis of α,β-substituted amino amides, esters, and acids 发明人:SHARPLESS K BARRY; RUBIN A ERIK 权利人:SCRIPPS RESEARCH INST 摘要:α,β-Unsaturated amides and esters are converted to α,β-substituted amino amides, esters, and acids. An α,βunsaturated amide or ester is first converted to an α,β-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The α,β-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a α,β-N-sulfonyl- or the α,β-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(α,β-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.