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573 results about "Propargyl" patented technology

In organic chemistry, propargyl is an alkyl functional group of 2-propynyl with the structure HC≡C−CH₂−, derived from the alkyne propyne. The term propargylic refers to a saturated position (sp³-hybridized) on a molecular framework next to an alkynyl group. The name comes from mix of propene and argentum, which refers to the typical reaction of the terminal alkynes with silver salts. The term homopropargylic designates in the same manner a saturated position on a molecular framework next to a propargylic group and thus two bonds from an alkyne moiety. a 3-butynyl fragment, HC≡C-CH₂CH₂-, or substituted homologue.

Neuroprotective iron chelators and pharmaceutical compositions comprising them

Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, eg. a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, a inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding ageing, and prevention and / or treatment of skin ageing and skin protection against sunlight and / or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety, the neuroprotective function is imparted to the compound e.g. by a neuroprotective peptide, and a combined antiapoptotic and neuroprotective function by a propargyl group.
Owner:TECHNION RES & DEV FOUND LTD +1

Preparation method and application of acid sensitive doxorubicin prodrug based on polyethylene glycol

The present invention provides an acid sensitive doxorubicin prodrug based on polyethylene glycol, and a method and an application of the acid sensitive doxorubicin prodrug based on polyethylene glycol. The preparation method comprises: preparing a polyethylene glycol whose end contains an acid sensitive acetal group and a p-nitrophenyl ester azide group by a reaction of a polyethylene glycol whose double ends contain diazido ethyl diacetal groups with a p-nitro phenyl propargyl carbonate; preparing the acid sensitive doxorubicin prodrug based on the polyethylene glycol by the reaction of the prepared polyethylene glycol with doxorubicin hydrochloride. The acid sensitive and water soluble doxorubicin prodrug has good biocompatibility and acid sensitivity, thereby being used as a stimulation sensitive antineoplastic prodrug.
Owner:SUZHOU UNIV

Method for preparing 1-propone-1,3-sultone

The invention relates to a method for preparing 1-propene-3-sultone, and the technical field of preparation of organic materials. The method mainly comprises the processes of addition, acidation and cyclization: a, addition, namely an addition reaction of propargyl ethanol and alkali metal sulphite or hydrosulfite is carried out in an aqueous solution, the molar ratio of the propargyl alcohol to the alkali metal sulphite or the hydrosulfite is 1:1-10, and inorganic acid or organic acid is added to stop reaction after the addition reaction is ended; and b, a product of the addition reaction isseparated out, and then the separated product is subjected to cyclization and separation to obtain a 1-propene-3-sultone product. The PST product can be refined. The method overcomes the defect of the prior art, and has the remarkable advantages of unique method, simple manufacturing process, easy operation, mild reaction conditions, cheap and easily-obtained raw materials, higher yield, good selectivity, high and stable quality of products, few three wastes, lower cost, remarkable economic benefit, and the like.
Owner:SHIJIAZHUANG SAN TAI CHEM CO LTD

Integrin ligand cyclic peptide analogues and cyclization method

The invention relates to a cyclopeptide analog and a cyclization method thereof, which aims at providing an integrin ligand cyclopeptide analog and a cyclization method thereof. The cyclization method comprises the following steps: Azido-glycine is firstly generated by glycin with the effects of trifluoromethanesulfonic anhydride and Sodium azide; Fmoc-Asp-Propargyl is then generated by condensation with propargylamine in solution; after side-chain carboxyl of propargyl acyl aspartic acid is then hung on 2-CTC resin, linear tetrapeptide analogs are condensed in turn, and the linear tetrapeptide analogs are then cut down from the resin; and the cyclopeptide analog is synthesized in the condition of liquid phase (DCM is used as a solvent and CuBr / DBU is used as catalyst) after 4 to 6 hours of reaction at room temperature. The cyclopeptide analog and cyclization method has the following advantages: (1) the integrin ligand cyclopeptide analog in the invention is introduced with heterocyclic rings (triazole rings), thereby being capable of increasing biological activity; and (2) the cyclization method in the invention is more simple, convenient and high-efficient, and the condition is moderate.
Owner:ZHEJIANG UNIV
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