6270-19-5

Usage

Chemical Properties

Colorless Transparent Liquid

InChI:InChI=1/C7H13NO2/c1-3-9-4-2-8(1)5-7-6-10-7/h7H,1-6H2/p+1/t7-/m1/s1

Upstream product

• 110-91-8 morpholine 
• 106-89-8 epichlorohydrin 
• 40893-69-4 1-chloro-3-(4-morpholinyl)-2-propanol 

Downstream Products

• 54743-12-3 1,3-bis-(2-hydroxy-3-morpholin-4-yl-propyl)-5,5-diphenyl-imidazolidine-2,4-dione 
• 54742-92-6 3-(2-hydroxy-3-morpholin-4-yl-propyl)-5,5-diphenyl-imidazolidine-2,4-dione 
• 61532-58-9 2-(N-Morpholinomethyl)-2H,3H-benzimidazo<1,2-b>oxazol 
• 92320-54-2 1-(2-chloro-6-methyl-anilino)-3-morpholin-4-yl-propan-2-ol 
• 35152-21-7 1-Butoxy-3-N-morpholino-2-propanol 
• 6425-32-7 3-morpholin-4-yl-propane-1,2-diol 
• 947394-05-0 3-(N-ethyl-N-phenylamino)-1-morpholinopropan-2-ol 
• 55212-21-0 1-morpholino-3-phenylaminopropan-2-ol 
• 135970-78-4 (S)-2-Benzyl-N-((2R,8S,11S,12R)-11-cyclohexylmethyl-12-hydroxy-2-morpholin-4-ylmethyl-5,9,13-trioxo-1-oxa-4,10-diaza-cyclotridec-8-yl)-3-(2-methyl-propane-2-sulfonyl)-propionamide 
• 135913-41-6 (S)-2-Benzyl-N-((2S,8S,11S,12R)-11-cyclohexylmethyl-12-hydroxy-2-morpholin-4-ylmethyl-5,9,13-trioxo-1-oxa-4,10-diaza-cyclotridec-8-yl)-3-(2-methyl-propane-2-sulfonyl)-propionamide 
• 135970-68-2 [(S)-1-((2R,8S,11S,12R)-11-Cyclohexylmethyl-12-hydroxy-2-morpholin-4-ylmethyl-5,9,13-trioxo-1-oxa-4,10-diaza-cyclotridec-8-ylcarbamoyl)-2-phenyl-ethyl]-carbamic acid tert-butyl ester 
• 135970-67-1 [(S)-1-((2S,8S,11S,12R)-11-Cyclohexylmethyl-12-hydroxy-2-morpholin-4-ylmethyl-5,9,13-trioxo-1-oxa-4,10-diaza-cyclotridec-8-ylcarbamoyl)-2-phenyl-ethyl]-carbamic acid tert-butyl ester 
• 141395-91-7 (4S,5R)-4-Cyclohexylmethyl-2,2-dimethyl-oxazolidine-3,5-dicarboxylic acid 5-{(R)-1-[((S)-4-benzyloxycarbonylamino-4-tert-butoxycarbonyl-butyrylamino)-methyl]-2-morpholin-4-yl-ethyl} ester 3-tert-butyl ester 
• 135913-05-2 (4S,5R)-4-Cyclohexylmethyl-2,2-dimethyl-oxazolidine-3,5-dicarboxylic acid 5-{(S)-1-[((S)-4-benzyloxycarbonylamino-4-tert-butoxycarbonyl-butyrylamino)-methyl]-2-morpholin-4-yl-ethyl} ester 3-tert-butyl ester 

Relevant academic research and scientific papers

Preparation method of 3-hydrazino-5-morpholinomethyl-2-oxazolidinone

The invention provides a preparation method of 3-hydrazino-5-morpholinomethyl-2-oxazolidinone, and belongs to the technical field of chemical synthesis. The preparation method comprises the followingsteps: carrying out a cyclization reaction on 1-Boc protective hydrazine-3-morpholine-2-propanol and a carbonic ester substance to obtain 3-Boc protective hydrazine-5-morpholinomethyl-2-oxazolidinone;and finally hydrolyzing to obtain the AMOZ. The chemical structural formula of the 1-Boc protective hydrazine-3-morpholine-2-propanol is shown in the specification, the chemical structural formula ofthe 3-Boc protective hydrazine-5-morpholinomethyl-2-oxazolidinone is shown in the specification, and the chemical structural formula of the AMOZ is shown in the specification; and the carbonic estersubstance contains at least one of diethyl carbonate, dimethyl carbonate, di-tert-butyl decarbonate, and dipropyl carbonate. The method is simple in synthetic route, the AMOZ is synthesized by adopting a one-pot method, and the catalyst is used in the preparation process, so that the loss in the synthesis process is greatly reduced, the synthesis yield and the recovery rate are relatively high; and the method is suitable for mass production.

Homopiperazine derived female controlled vaginal trichomonacidal contraceptive: An addition to structure-activity relationship

Background: In our previous work, several piperazine derived bis(dialkylaminethiocarbonyl) disulfides and disulfide esters of dithiocarbamic acid have been synthesized and evaluated for their spermicidal and microbicidal efficacy. These studies have provided some promising compounds for developing a dually active vaginal microbicidal contraceptive which is under pre-clinical stage. Objective: The main objective of this study was the design synthesis and biological evaluation of bis(dialkylaminethiocarbonyl) disulfides (4–15) and 2,2’-disulfanediylbis (3-(substituted-1-yl) propane-2,1-diyl) disubstituted-1-carbodithioates (19-28) as non-surfactant molecules capable of eliminating Trichomonas vaginalis as well as irreversibly immobilizing 100% human sperm promptly. Method: Spermicidal, anti-trichomonas, cytotoxicity and biocompatibility study of the synthesized compounds was done as per the reported methodologies. Result: Among bis(dialkylaminethiocarbonyl) disulfides (4-15, Table 1), compound 4 (MEC 0.02 mM) was found to be the most desirable for spermicidal activity as it was 40 times more active than Nonoxynol-9 (N-9), and also active against Trichomonas vaginalis (MIC 0.02 &1.10 mM). 2, 2’-disulfanediylbis (3-(substituted-1-yl) propane-2, 1-diyl) disubstituted-1-carbodithioates (19-28, Table 2), and compounds (19, 22, 23, and 24 MEC 0.05 mM) were sixteen times more active than N-9 with promising Trichomonacidal activity. Conclusion: This study suggested that the disulfide linkage alone and dithiocarbamate along with disulfide group within the same chemical entity impart the desired multiple activities of compounds.

Innovative Disulfide Esters of Dithiocarbamic Acid as Women-Controlled Contraceptive Microbicides: A Bioisosterism Approach

In an ongoing effort to discover an effective, topical, dual-function, non-surfactant contraceptive vaginal microbicide, a novel series of 2,2′-disulfanediylbis(3-(substituted-1-yl)propane-2,1-diyl) disubstituted-1-carbodithioates were designed by using a bioisosterism approach. Thirty-three compounds were synthesized, and interestingly, most demonstrated multiple activities: they were found to be spermicidal at a minimal effective concentration of 1-0.001 %, trichomonacidal against drug-susceptible and resistant Trichomonas strains at minimal inhibitory concentration (MIC) ranges of 10.81-377.64 and 10.81-754.14 μM, respectively, and fungicidal at MIC 7.93-86.50 μM. These compounds were also found to be non-cytotoxic to human cervical (HeLa) epithelial cells and vaginal microflora (Lactobacilli) in vitro. The most promising compound, 2,2′-disulfanediylbis(3-(pyrrolidin-1-yl)propane-2,1-diyl)dipyrrolidine-1-carbodithioate (5), exhibited spermicidal activity 15-fold higher than that of the marketed spermicide Nonoxynol-9 (N-9) and also demonstrated microbicidal potency. To identify common structural features required for spermicidal activity, a 3D-QSAR analysis was carried out, as well as in vivo efficacy studies and fluorescent labeling studies to determine the biological targets of compound 5. Change it out: A series of disulfide esters of dithiocarbamic acid were synthesized to block free sulfhydryl groups present in sperm and Trichomonas for a safe dual-action spermicide. A majority of the compounds demonstrated multiple activities with good safety profiles, with the most promising compound exhibiting spermicidal activity 15-fold higher than that of the marketed spermicide Nonoxynol-9.

Metal free synthesis of morpholine fused [5,1-c] triazolyl glycoconjugates via glycosyl azido alcohols

A series of diverse glycosyl 1,2-azido alcohols, obtained from readily available carbohydrates, were converted to structurally varied rare and novel sugar derived morpholine fused [5,1-c]-triazoles via a one-pot strategy. After incorporating a propargyl functionality at the hydroxyl group of the sugar derived 1,2-azido alcohols, the resulting in situ generated azido-alkyne affords numerous C- and O-glycosyl bicyclic ring systems with medicinal value via a metal free cycloaddition reaction. The structures of all the developed molecules have been elucidated using 1H NMR, 13C NMR, IR and MS spectroscopy.

PYRROLO-NITROGENOUS HETEROCYCLIC DERIVATIES,THE PREPARATION AND THE PHARMCETICAL USE THEEOF

The invention provides new pyrrolo-nitrogenous heterocyclic derivatives represented by formula (I) or their salts, the preparation thereof, pharmaceutical compositions containing such derivatives and the use of such derivatives as therapeutic agents, especially as protein kinase inhibitors, wherein each substituent in formula (I) is same as defined in the description.

Synthesis of the hypotensive agent 8-amino-7-[2-hydroxy-3-morpholinopropyl] theophylline (P23) and analogs

Synthesis of a number of 7, 8-disubstituted theophyllines including enantiomers of the hypotensive agent P23 is described.

Syntheses on the basis of 4-(oxiran-2-ylmethyl)morpholine

4-(Oxiran-2-ylmethyl)morpholine was synthesized and converted into new morpholino derivatives of propan-2-ols and butan-4-olides.

Structure and Reactivity of Oxirane Chemical Modifiers for Gelatin

New chemical modifiers for gelatin, glycidylamines, are synthesized.Acid-base properties of glycidylamines and the kinetics of reactions of oxirane compounds with nucleophilic reagents, among them aqueous solution of gelatin, are studied.

NEW RENIN-INHIBITORY OLIGOPEPTIDES, THEIR PREPARATION AND THEIR USE

Oligopeptides of formula (I): STR1 where R 1-R 5 are various organic groups, and A represents a group of formula--NH--or--(CH 2) n--, in which n represents an integer of from 1 to 3, have renin-inhibitory activity and are particularly suitable for oral administration. They may be prepared by condensing their component amino acids or lower oligopeptides using conventional peptide synthesis reactions.