104882-10-2

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 104882-45-3 (S)-2-amino-1-cyclohexyl-(R)-3,(S)-4-dihydroxy-6-methylheptane hydrochloride 
• 122621-77-6 (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane 
• 131550-34-0 (S)-2-Cyclohexyl-1-((4R,5S)-5-isobutyl-2,2-dimethyl-[1,3]dioxolan-4-yl)-ethylamine 
• 114457-87-3 (2S,3R)-2-<(tert-butyloxycarbonyl)amino>-1-cyclohexyl-3-hydroxy-6-methylheptan-4-one 
• 141364-52-5 (4S,5S)-2,2-Dimethyl-4-(2-methylpropyl)-5-formyl-1,3-dioxolane dimethyl hydrazone 
• 117161-13-4 (4S,5R)-4-cyclohexylmethyl-5-<(1'S)-1'-hydroxy-3-methylbutyl>oxazolidin-2-one 
• 131451-93-9 (4S,5R)-3-Benzyl-4-cyclohexylmethyl-5-<(R)-(2-benzyloxy-1-methanesulfonyloxy)ethyl>oxazolidin-2-one 
• 131451-94-0 (4S,5R)-3-Benzyl-4-cyclohexylmethyl-5-<(R)-(2-hydroxy-1-methanesulfonyloxy)ethyl>oxazolidin-2-one 
• 131451-97-3 (4S,5R)-3-Benzyl-4-cyclohexylmethyl-5-<(S)-(1-hydroxy-3-methyl)butyl>oxazolidin-2-one 
• 131451-95-1 (4S,5R)-3-Benzyl-4-cyclohexylmethyl-5-<(S)-oxiran-2-yl>oxazolidin-2-one 
• 139056-96-5 (4R,5R)-4-<(S)-(1-(N-Benzyl-N-methoxycarbonyl)amino-2-cyclohexyl)ethyl>-5-benzyloxymethyl-2,2-dimethyl-1,3-dioxolane 
• 139056-97-6 (2R,3R,4S)-4-(N-Benzyl-N-methoxycarbonyl)amino-1-benzyloxy-5-cyclohexylpentane-2,3-diol 
• 130914-06-6 (4R,5R)-4-<(S)-(1-N-Benzylamino-2-cyclohexyl)ethyl>-5-benzyloxymethyl-2,2-dimethyl-1,3-dioxolane 

Downstream Products

• 144599-41-7 (2S,3R,4S)-2-(N-Boc-Isoleucyl-Isoleucyl-Amino)-1-cyclohexyl-3,4-dihydroxy-6-methylheptane 
• 127254-98-2 (2S,3R,4S)-1-cyclohexyl-3,4-dihydroxy-6-methyl-2-<(p-tolylsulfonyl)amino>heptane 
• 140926-08-5 (2S,3R,4S)-2-<-3-(4-thiazolyl)-L-alanyl>amino>-1-cyclohexyl-3,4-dihydroxy-6-methylheptane 
• 141115-19-7 (S)-2-Benzyl-N-[(S)-1-((1S,2R,3S)-1-cyclohexylmethyl-2,3-dihydroxy-5-methyl-hexylcarbamoyl)-2-thiazol-4-yl-ethyl]-4-morpholin-4-yl-4-oxo-butyramide 
• 141042-01-5 (1S,2S,3S)-2-Isobutyl-3-(morpholine-4-carbonyl)-cyclopropanecarboxylic acid [(S)-1-((1S,2R,3S)-1-cyclohexylmethyl-2,3-dihydroxy-5-methyl-hexylcarbamoyl)-2-thiazol-4-yl-ethyl]-amide 
• 141042-05-9 (1S,2R,3S)-2-Isobutyl-3-(morpholine-4-carbonyl)-cyclopropanecarboxylic acid [(S)-1-((1S,2R,3S)-1-cyclohexylmethyl-2,3-dihydroxy-5-methyl-hexylcarbamoyl)-2-thiazol-4-yl-ethyl]-amide 
• 141041-98-7 (1R,2S,3R)-2-Isobutyl-3-(morpholine-4-carbonyl)-cyclopropanecarboxylic acid [(S)-1-((1S,2R,3S)-1-cyclohexylmethyl-2,3-dihydroxy-5-methyl-hexylcarbamoyl)-2-thiazol-4-yl-ethyl]-amide 
• 140903-51-1 (1R,2R,3R)-2-Isobutyl-3-(morpholine-4-carbonyl)-cyclopropanecarboxylic acid [(S)-1-((1S,2R,3S)-1-cyclohexylmethyl-2,3-dihydroxy-5-methyl-hexylcarbamoyl)-2-thiazol-4-yl-ethyl]-amide 
• 141042-00-4 (1S,2S,3S)-2-Ethyl-3-(morpholine-4-carbonyl)-cyclopropanecarboxylic acid [(S)-1-((1S,2R,3S)-1-cyclohexylmethyl-2,3-dihydroxy-5-methyl-hexylcarbamoyl)-2-thiazol-4-yl-ethyl]-amide 

Relevant academic research and scientific papers

A diastereoselective synthesis of (2S, 3R, 4S)-2-amino-1-cyclohexyl-6-methylheptane-3,4-diol, the Abbott aminodiol

An efficient asymmetric synthesis of the Abbott aminodiol, 1, is described beginning with the readily-available starting material, L-phenylalanine.

USE OF ETHYNYL ALANINE AMINO DIOL COMPOUNDS FOR TREAMENT OF OPHTHALMIC DISORDERS

Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. Compounds of particular interest are those of Formula I STR1 wherein A is selected from CO and SO 2 where

Enantioselective synthesis of the (syn,anti)-1-amino-2,3-diol subunit of renin inhibition by reaction of β-lactams with a Grignard reagent

A new approach to the BOC-protected amino diol 1a via the opening of 3,4-cis-disubstituted β-lactam 3 with isobutylmagnesium chloride is described. Nonracemic β-lactam 3 could be obtained by enzymatic resolution of the 3-acetoxy-β-lactam 4 or from a chira

ALKYLAMINOALKYL-TERMINATED SULFIDE/SULFONYL-CONTAINING PROPARGYL AMINO-DIOL COMPOUNDS FOR TREATMENT OF HYPERTENSION

Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: STR1 wherein q is two or three; wherein r is zero or two; wherein R 2 is selected from hydrido, methyl, ethyl and phenyl; wherein R 3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R. sup.5 is propargyl or a propargyl containing moiety; wherein R. sup.7 is cyclohexylmethyl; wherein R 8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R. sup.12 and R 13 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.

3-AZABICYCLO[3.2.1]-NONANYL-TERMINATED NON-PIPTIDYL ALPHA-SUCCINAMIDOACYL AMINODIOLS AS ANTI-HYPERTENSIVE AGENTS

Non-peptidyl compounds characterized generally as α-succinamidoacyl aminodiols having a 3-azabicyclo[3.2.2]-nonanyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.

Diastereoselectivity in the osmium-catalyzed dihydroxylation of allylic amides and carbamates

The stereochemistry of the osmium-catalyzed dihydroxylation of a series of chiral allylic amides and carbamates has been studied. The diastereoselectivity of these reactions was found to be dependent upon the solvent and the nitrogen protecting group as w

ETHYNYL ALANINE AMINO DIOL COMPOUNDS HAVING A PIPERAZINYL-TERMINATED GROUP OR A PIPERAZINYL-ALKYLAMINO-TERMINATED GROUP FOR TREATMENT OF HYPERTENSION

Compounds characterized generally as ethynyl alanine amino diol compounds having a piperazinyl-terminated or a piperazinyl-alkylamino-terminated group and derivatives thereof are useful as renin inhibitors for the treatment of hypertension. Compounds of p

Imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension

Compounds characterized generally as imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I STR1 wher

CYCLOPROPYL-ALANINE ARYL/ALKYLSULFIDE/SULFONYL-TERMINATED AMINO-DIOL COMPOUNDS FOR TREATMENT OF HYPERTENSION

Compounds characterized generally as cyclopropyl alanine aryl/alkylsulfide/sulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula STR1 wherein

Potent and Selective Inhibitors of an Aspartyl Protease-like Endothelin Converting Enzyme Identified in Rat Lung

Two structurally distinct series of potent and selective inhibitors of an aspartyl protease-like endothelin converting enzyme (ECE) activity identified in the rat lung have been developed.Pepstatin A, which potently inhibits the rat lung ECE, served as the basis for the first series.Alternatively, selected renin inhibitors containing the dihydroxyethylene moiety were shown to be inhibitors of rat lung activity.Subsequent modifications improved inhibition of the rat lung ECE while eliminating renin activity.Both series of ECE inhibitors demonstrated a range of selectivity over Cathepsin D.Water-solubilizing moieties were appended onto selected compounds to facilitate in vivo testing.Partial reduction of the pressor response to exogenously administered Big ET-1 was observed with selected rat lung ECE inhibitors.