321386-75-8

Upstream product

• 25125-21-7 4-(hydroxymethyl)cyclopentene 
• 7143-01-3 Methanesulfonic anhydride 
• 124-63-0 methanesulfonyl chloride 

Downstream Products

• 4492-42-6 (cyclopent-3-ene)methylamine 
• 207729-05-3 tert-butyl cyclopent-3-enylmethylcarbamate 
• 910223-55-1 4-cyclopent-3-enyl-2-diazo-3-oxo-butyric acid 2-oxo-1-phenyl-2-pyrrolidin-1-yl-ethyl ester 
• 910223-57-3 2-oxo-1,2,3,3a,4,6a-hexahydro-pentalene-1-carboxylic acid 2-oxo-1-phenyl-2-pyrrolidin-1-yl-ethyl ester 

Relevant academic research and scientific papers

Preparation method and intermediate of fused tricyclic derivative

The invention provides a preparation method of a fused tricyclic derivative intermediate. The intermediate has a structure shown as a formula (4-7). The preparation method has the advantages of accessible raw materials and simple steps and is suitable for large-scale industrial production.

Desymmetrization of cyclic olefins via asymmetric Heck reaction and hydroarylation

An asymmetric Heck reaction allows desymmetrization of substituted cyclic olefins in high dr and ee. A bisphosphine oxide is uniquely stereoselective for this purpose. Desymmetrization of bicyclic olefins via hydroarylation can also be realized in high ee.

Pleuromutilin derivatives for use in the treatment of diseases mediated by microbes

Compounds selected from the group ofN-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyt-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.

PLEUROMUTILIN DERIVATIVES FOR USE IN THE TREATMENT OF DISEASES MEDIATED BY MICROBES

Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy- cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)- acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.

Synthetic studies on altemicidin: Stereocontrolled construction of the core framework

(Chemical Equation Presented) The stereoselective synthesis of the key intermediate for altemicidin has been accomplished. The synthesis commenced with a bicyclo[3.3.0] framework, which was readily obtained via an intramolecular C-H insertion reaction. A Curtius rearrangement was employed as a key step to stereoselectively construct the β-hydroxyl α-disubstituted-α- amino acid structure. Synthesis of vinylogous urea was achieved using hydrolysis of nitrile intermediate.

A novel synthesis of bicyclo[3.3.0]octane ring system via a desymmetric C-H insertion reaction

An optically active bicyclo[3.3.0]octane ring was synthesized by an intramolecular C-H insertion reaction. Upon treatment with a catalytic amount of Rh2(S-DOSP)4, a chiral-auxiliary-containing diazoester underwent a C-H insertion reaction to give the desired bicyclo[3.3.0]octane system. Georg Thieme Verlag Stuttgart.

Total synthesis of (+/-)-cytisine via the intramolecular heck cyclization of activated N-alkyl glutarimides.

[reaction:see text] A synthesis of racemic cytisine 1 has been developed utilizing an intramolecular Heck cyclization to prepare the bridged tricyclic intermediate 2. The cyclization employs activated glutarimide-derived ketene aminals 3 (X = P(O)OEt(2) or SO(2)CF(3)) and represents the first use of such intermediates in metal-catalyzed processes.