专利号:US-2009198084-A1 优先权日:2006-05-02 标题:Process for the deprotection of protected amines 发明人:ALSTERS PAULUS LAMBERTUS; VERKADE JORGE MERIJN MATHIEU; QUAEDFLIEG PETER JAN LEONARD MARIO; RUTJES FLORIS PETRUS JOHANNES 权利人:ALSTERS PAULUS LAMBERTUS; VERKADE JORGE MERIJN MATHIEU; QUAEDFLIEG PETER JAN LEONARD MARIO; RUTJES FLORIS PETRUS JOHANNES 摘要:The present invention relates to a process for the deprotection of protected amine compounds, wherein the protected amine compound is contacted with an electrophilic oxidating agent that is optionally formed in situ, said electrophilic oxidating agent being selected from the group of I 2 , Br 2 , Cl 2 and compounds comprising a halogen atom having a formal oxidation state of 1+, 3+, 5+ or 7+, provided that the electrophilic oxidating agent is not iodobenzene diacetate. The process can be conveniently employed in the synthesis of 1,3-amino alcohols, β-amino acids and heterocyclic compounds, in particular β-amino acids.
专利号:US-6720439-B1 优先权日:2001-09-28 标题:Synthesis of ruthenium-hydride complexes and preparation procedures of chiral alcohols and ketones 发明人:OHKUMA TAKESHI; KOIZUMI MASATOSHI; MUNIZ KILIAN; NOYORI RYOJI 权利人:INST NAGOYA IND SCIENCE RES 摘要:trans-RuH(eta<1>-BH4)[(S)-xylbinap][(S,S)-dpen] (0.00125 mmol), acetophenone (5.0 mmol), and 2-propanol (2.5 mL) were placed in an autoclave, and the resulting solution was repeatedly subject 5 times to a procedure of performing pressure reduction and argon introduction while stirring the solution for deaeration. A hydrogen tank was then connected to the autoclave, and after replacing the air inside an introduction tube with hydrogen, the pressure inside the autoclave was adjusted to 5 atmospheres and then hydrogen was released until the pressure dropped to 1 atmosphere. After repeating this procedure 10 times, the hydrogen pressure was adjusted to 8 atmospheres and stirring at 25° C. was performed for 12 hours. By concentrating the solution obtained by depressurization and subjecting the crude product to simple distillation, (R)-1-phenylethanol (yield: 95%) in the form of a colorless oily substance was obtained at an ee of 99%.
专利号:WO-2012024104-A2 优先权日:2010-08-16 标 题 :Biocatalysts and methods for the synthesis of (1r,2r)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine
专利号:US-4663474-A 优先权日:1983-02-22 标题 :Synthetic intermediates for a chiral 3-(substituted-phenyl)-4-(3-hydroxypropyl) cyclohexanol 发明人:URBAN FRANK J 权利人:PFIZER 摘要:Racemic endo- and exo-1-methoxybicyclo[2.2.2]oct-5-ene-2-carboxylic acids are starting materials for a novel and efficient synthesis of chiral 3R-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-4R-(3-hydroxypropyl)-1R-cyclohexanol, a compound having valuable central nervous system (CNS) activity, particularly as an analgesic and as an antiemetic.