📜Cis-4-Aminocycloheptanol置于氯化亚砜体系中,用 氘代氯仿 用作溶剂,化学反应 26.5H,反应生成降莨菪鹼 参考文献:Synthetic Approaches To Nortropanes And Nortrop-6-Enes; Intramolecular Displacement By Nitrogen In 7-Membered Rings 标题:Synthetic Approaches To Nortropanes And Nortrop-6-Enes; Intramolecular Displacement By Nitrogen In 7-Membered Rings 摘要:The Synthesis Of Simple Nortropane And Nortrop-6-Ene Derivatives From Cyclohepta-1,3-Diene Is Described. The Key Intermediates Are Trans-1-Amino-4-Chloro-Cycloheptanes And-Cyclohept-2-Enes Which Are Derived Efficiently From The Corresponding Cis-Amino-Alcohols And Undergo Intramolecular Cyclisation. Corresponding Derivatisation Of Cyclohexa-And Cycloocta-1,3-Dienes Is Explored And Attempts To Achieve Pd-Catalysed Cyclisation Of 1-Amino-4-Acetoxy-Derivatives Is Described. Nitrogen Inversion Data For Selected Nortropane Derivatives Are Included. Doi:10.1016/s0040-4020(01)80313-6
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-11325912-B2 优先权日:2019-05-09 标题 :Regio-selective synthesis of imidazo[1,2-a]pyrimidines 发明人:CLAGG KYLE BRADLEY PASCUAL; WHITE NICHOLAS ANDREW; ZHANG HAIMING; GOSSELIN FRANCIS; NACK WILLIAM; O'SHEA PAUL D 权利人:GENENTECH INC 摘要:A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb)comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.
专利号:US-2024084295-A1 优先权日:2020-12-08 标 题:Novel Synthesis of Phosphorodithioate Oligonucleotides 发明人:BOLLMARK MARTIN; SEHGELMEBLE TORREJON WALTER FERNANDO; SLADOJEVICH FILIPPO; TEDEBARK ULF 权利人:HOFFMANN LA ROCHE 摘要:The invention provides the use of a compound of formula (I), as defined, for the preparation of an oligonucleotide comprising at least one phosphorodithioate internucleoside linkage. Various synthesis methods using compounds of formula (I) are provided.
专利号:WO-2023086801-A1 优先权日:2021-11-09 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-2023407293-A1 优先权日:2021-10-27 标 题:Dna-encoded and affinity-tagged masked-warhead compounds and use thereof in assembling libraries of small molecules enabled for late-stage purification and multiplexed screening of covalent ligands 发明人:MAIANTI JUAN PABLO 权利人:MAIANTI JUAN PABLO 摘要:The present disclosure relates to DNA-encoded and affinity-tagged masked warhead installation compounds and use thereof in the synthesis of electrophilic warhead DNA-Encoded Libraries (eDEL), including substituted and unsubstituted acrylamide warheads, which can be purified from unreacted library intermediates and byproducts.
专利号:US-10906895-B2 优先权日:2017-02-16 标 题:Processes for the preparation of benzodiazepine derivatives 发明人:KIM IN JONG; YU JIANMING; BLAISDELL THOMAS P; Panarese Joseph; SHOOK BRIAN C; OR YAT SUN 权利人:ENANTA PHARM INC 摘要:The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of Respiratory Syncytial Virus (RSV) inhibitors. The present invention also relates to processes and intermediates for the preparation of compounds of formula (I): n n n n n n n n n n In particular, the present invention also relates to processes and intermediates for the preparation of compound I-a:
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