CAS: 155-09-9; Tranylcypromine

相似化合物

1986-47-6 3721-28-6 37388-05-9

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-5877278-A
优先权日:1992-09-24
标题:Synthesis of N-substituted oligomers
发明人：ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.

专利号:US-4016204-A
优先权日:1975-10-31
标 题 :Method of synthesis of trans-2-phenylcyclopropylamine
发明人：RAJADHYAKSHA VITHAL JAGANNATH
权利人:NELSON RES & DEV
摘要:An improved method of synthesis of trans-2-phenylcyclopropylamine wherein the improvement comprises isomerizing an intermediate ester, namely, cis,trans-ethyl-2-phenylcyclopropanecarboxylate, by reacting said ester with anhydrous sodium ethoxide, to form a reaction product containing not more than about 5 percent cis ester and further reacting said resultant product to form trans-2-phenylcyclopropylamine.

专利号:EP-3617181-A1
优先权日:2018-08-30
标题:Synthesis of trans-2-phenylcyclopropylamine or a salt or solvate thereof
发明人：BREUNING ALEXANDER; LIMMERT MICHAEL; DELLING AXEL; HOFMEIER HARALD; HULTSCH JANA; MICKSCH MAIK; SOMMER CHRISTIAN
权利人:AREVIPHARMA GMBH
摘要:The present invention relates to the field of manufacturing trans-2-phenylcyclopropylamine or a salt or solvate thereof, in particular in the form of the sulphate salt. The obtained product, particularly when in the form of the synthesis of trans-2-phenylcyclopropylamine sulphate, is exceptionally pure, substantially free from reactants and reagents that are mutagenic, hazardous or of great concern to the health of humans or the environment.

专利号:US-12234200-B2
优先权日:2019-04-16
标 题:Synthetic methods of preparing esketamine
发明人：CHEN CHENG YI
权利人:JANSSEN PHARMACEUTICA NV
摘要:The present invention is directed to methods for the asymmetric synthesis of esketamine. The present invention is further directed to key intermediates in the asymmetric esketamine synthesis. In one embodiment, the invention is an asymmetric synthesis of esketamine comprising the conversion of (S)-2′-chloro-2-methoxy-3,4,5,6-5 tetrahydro-[1, 1′-biphenyl]-3-yl carbamate to (S)-2′-chloro-1-isocyanato-6-methoxy-1,2,3,4-tetrahydro-1,1′-biphenyl.

专利号:US-2007082943-A1
优先权日:2005-04-01
标 题:Process for preparation of substantially pure glimepiride
发明人：KADAM SURESH M; TARUR VENKATASUBRAMANIAN R; NAIK SANJAY J; GAVHANE SACHIN B
权利人:KADAM SURESH M; TARUR VENKATASUBRAMANIAN R; NAIK SANJAY J; GAVHANE SACHIN B
摘要:The present invention discloses a novel process for purification of trans-4-methyl cyclohexylamine HCl and 4[-2-(3-Ethyl-4-methyl-2-carbonyl pyrrolidine amido) ethyl] benzene sulfonamide used in the synthesis of 3-Ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(trans-4-methyl cyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide (I), popularly known as Glimepiride. The present invention also discloses a novel purification of Glimepiride usingS methanolic ammonia and glacial acetic acid to obtain highly pure Glimepiride Form I (I) having the undesired cis isomer below 0.15%. Glimepiride (I) is useful in the treatment of diabetes mellitus.