40226-04-8

Upstream product

• 138286-76-7 ethyl-2-bromooctanoate 
• 122-52-1 triethyl phosphite 
• 867-13-0 diethoxyphosphoryl-acetic acid ethyl ester 
• 638-45-9 1-Iodohexane 
• 124-07-2 Octanoic acid 
• 111-25-1 1-bromo-hexane 

Downstream Products

• 35045-86-4 α-aminoheptanephosphonic acid 
• 1414882-83-9 (2E,4Z)-tert-butyl 6-benzylamino-5-hexyl-6-oxohexa-2,4-dienoate 
• 1414882-74-8 N-methoxyl-N-methyl-N’-benzyl-5-hexyl-hexa-2E,4Z-diendiamide 
• 1414882-57-7 (2E,4Z)-n-butyl 6-benzylamino-5-hexyl-6-oxohexa-2,4-dienoate 
• 177587-26-7 N-t-butoxycarbonyl-1-hexyl-2-[4-methoxy-3-(2-phenylethoxy)-phenyl]ethylamine 
• 177587-43-8 1-(4-methoxy-3-phenethyloxy-benzyl)-heptylamine 

Relevant academic research and scientific papers

Stereo- and chemoselective cross-coupling between two electron-deficient acrylates: An efficient route to (Z, E)-muconate derivatives

A Ru-catalyzed direct oxidative cross-coupling reaction of acrylates was developed. It offers a straightforward and atom-economical protocol for the synthesis of functionalized (Z,E)-muconate derivatives in moderate to good yields with good stereo- and chemoselectivities. The conjugated muconates bearing differentiable terminal functionality can be selectively transformed into versatile synthetic intermediates widely used in organic synthesis.

Rhodium(III)-catalyzed olefinic C-H alkynylation of acrylamides using tosyl-imide as directing group

The Rh(III)-catalyzed C-H alkynylation of acrylamide derivative is realized using a hypervalent alkynyl iodine reagent. The use of a weakly coordinating directing group proved to be of critical importance. This reaction displays broad functional group tolerance and high efficiency, which opens a new synthetic pathway to access functionalized 1,3-enyne skeletons.

Synthesis and characterization of novel phosphonocarboxylate inhibitors of RGGT

Phosphonocarboxylate (PC) analogs of the anti-osteoporotic drugs, bisphosphonates, represent the first class of selective inhibitors of Rab geranylgeranyl transferase (RabGGTase, RGGT), an enzyme implicated in several diseases including ovarian, breast and skin cancer. Here we present the synthesis and biological characterization of an extended set of this class of compounds, including lipophilic derivatives of the known RGGT inhibitors. From this new panel of PCs, we have identified an inhibitor of RGGT that is of similar potency as the most active published phosphonocarboxylate, but of higher selectivity towards prenyl pyrophosphate synthases. New insights into structural requirements are also presented, showing that only PC analogs of the most potent 3rd generation bisphosphonates inhibit RGGT. In addition, the first phosphonocarboxylate-derived GGPPS weak inhibitor is reported.

Directing-group-assisted copper-catalyzed olefinic trifluoromethylation of electron-deficient alkenes

Assistance provided: The directing group in the title reaction not only activates the substrates but also allows the stereospecific formation of cis-trifluoromethylated products. The reaction is operationally simple and tolerates a wide variety of functional groups, thus providing an efficient method for the stereoselective synthesis of β-CF3-functionalized acrylamide derivatives. Copyright

Ruthenium- and rhodium-catalyzed cross-coupling reaction of acrylamides with alkenes: Efficient access to (Z,E)-dienamides

Ruthenium- and rhodium-catalyzed direct oxidative cross-coupling reactions of acrylamides with alkenes were developed. These methods provide an efficient route for the synthesis of (Z,E)-dienamides in excellent yields with good stereoselectivity. The catalytic systems allowed oxidative olefination of a wide range of alkenes bearing different functional groups, such as CO2R, COMe, SO2Ph, aryl, CONHBn, CN, PO(OEt)2, as well as Weinreb amide.

Synthesis of anti-Alzheimer (R)-arundic acid

The asymmetric synthesis of the anti-Alzheimer agent (R)-arundic acid has been performed via a diastereoselective photodeconjugation reaction as the key-step. The synthetic approach involves a readily available chiral auxiliary, diacetone-d-glucose, and allows access to either enantiomer as illustrated by the synthesis of (S)-arundic acid. Both enantiomers were obtained in 88% ee using the same chiral auxiliary.

Synthesis and SAR of 1-alkyl-2-phenylethylamine derivatives designed from N,N-dipropyl-4-methoxy-3-(2-phenylethoxy)phenylethylamine to discover σ1 ligands

The synthesis and structure-activity relationships (SAR) of 1-alkyl-2- phenylethylamine derivatives 5-8 designed from N,N-dipropyl-2-[4-methoxy-3- (2-phenylethoxy)phenyl]ethylamine hydrochloride (1, NE-100) are presented. The SAR between compound 1 and 1-alkyl-2-phenylethylamine derivatives suggested that the alkyl group on the 1-position carbon of 2-[4-methoxy-3-(2- phenylethyl)phenyl]ethylamine derivatives played the role of one of the propyl groups on the aminic nitrogen of compound 1. (-)-N-Propyl-1-butyl-2- [4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine hydrochloride ((-)-6d, NE-537) and (-)-N-propyl-1-(3-methybutyl)-2-[4-methoxy-3-(2- phenylethoxy)phenyl]ethylamine hydrochloride ((-)-6i, NE-535), typical compounds in this series, have potent and selective σ1 affinity.

Thiol based collagenase inhibitors

This invention relates to compounds of the formula: STR1 wherein R 1 represents lower alkyl, phenyl or phenyl lower alkyl;R 2 and R 4 represent lower alkyl; andR 3 represents lower alkyl, benzyloxyalkyl, alkoxybenzyl or benzyloxybenzyl wherein the oxyalky