2276 results about "Alkyl substitution" patented technology

New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.

A photoacid compound having the following general structure:<paragraph lvl="0"><in-line-formula>R-O(CF2)nSO3X</in-line-formula>wherein n is an integer between about 1 to 4; R is selected from the group consisting of: substituted or unsubstituted C1-C12 linear or branched alkyl or alkenyl, substituted or unsubstituted araalkyl, substituted or unsubstituted aryl, substituted or unsubstituted bicycloalkyl, substituted or unsubstituted tricycloalkyl, hydrogen, alkyl sulfonic acid, substituted or unsubstituted perfluoroalkyl, the general structure F((CF2)pO)m(CF2)q- wherein p is between about 1 to 4, m is between about 0 to 3 and q is between about 1 to 4, and substituted or unsubstituted partially fluorinated alkyl, halofluoroalkyl, perfluoroalkylsulfonic, or glycidyl; and X is selected from the group consisting of: organic cations and covalently bonded organic radicals.

The invention provides a preparation method of ticagrelor, belonging to the technical field of medicine manufacturing. According to the method, a compound VII is taken as a raw material, and the method comprises the steps of: carrying out a nucleophilic substitution reaction on the raw material to obtain a compound VI; hydrogenating the VI, removing carbamazepine (Cbz) protection to obtain a compound V; carrying out a reaction on the V and 4, 6-dichloro-2-(allyl sulfide)-5-amio-pyrimidine to obtain a compound IV; carrying out a reaction on the IV and nitrite of alkali metal to obtain a compound III; carrying out a reaction on the III and (1R, 2S)-2-(3, 4-difluoro phenyl) cyclopropylamine to obtain a compound II; and finally, removing protecting group of the II to obtain a compound I.

The present invention relates to a compound represented by Formula (1) and a polymer obtained using the compound:

wherein R¹ is phenyl which may have substituents, Q¹ is hydrogen, halogen, alkyl having 1 to 10 carbon atoms, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl or phenyl in which optional hydrogen may be replaced by halogen or alkyl having 1 to 5 carbon atoms,

and Q² is a group represented by Formula (2) wherein the code < represents a bonding point with silicon, l, m, n and p are independently 0, 1, 2 or 3, A¹ to A⁴ are independently a single bond, 1,4-cyclohexylene, 1,4-cyclohexenylene, a condensed ring group having 6 to 10 carbon atoms which is a divalent group, or 1,4-phenylene, Z⁰ to Z³ are independently a single bond, —CH═CR—, —C≡C—, —COO—, —OCO—, or alkylene having 1 to 20 carbon atoms, and Z⁴ is a single bond, —CH═CH—, —C≡C—, —COO—, —OCO—, or alkylene having 1 to 20 carbon atoms. And Y¹ in Formula (1) is the group defined in Claim 1.

An overbased, sulfurized salt of at least one alkylated hydroxyaromatic compound, wherein the alkyl substituent of the hydroxyaromatic compound is a residue of at least one isomerized olefin having from about 15 to about 99 wt. % branching is disclosed. The overbased, sulfurized salt of at least one alkylated hydroxyaromatic compound is produced by the process comprising: (a) alkylating at least one hydroxyaromatic compound with at least one isomerized olefin having from about 15 to about 99 wt. % branching obtained by isomerizing at least one normal alpha olefin having from about 10 to about 40 carbon atoms, to provide at least one alkylated hydroxyaromatic compound; (b) neutralizing and sulfurizing the alkylated hydroxyaromatic compound in any order to provide at least one neutralized, sulfurized alkylated hydroxyaromatic compound; and (c) overbasing the at least one neutralized, sulfurized alkylated hydroxyaromatic compound.

The invention discloses a C3/C3 fluoroquinolone dimmer derivative using oxadiazole as a connection chain as well as a preparation method and an application thereof. The C3/C3 fluoroquinolone dimmer derivative using oxadiazole as a connection chain is a compound which has the following structural general formula (I), wherein R1 and R1' are independently selected from H, (C1-C10) alkyl, (C3)-(C10) cycloalkyl, (C1)-(C10) haloalkyl and substituted aryl group or substituted heterocyclic aryl group; R2 and R2' are independently selected from H, (C1-C7)alkyl, (C3)-(C7) cycloalkyl, substituted aryl group, substituted heterocyclic aryl group and hydrocarbon acyl or sulfonyl; R3 and R3' are independently selected from H, (C1-C5) alkyl, (C3)-(C5) cycloalkyl, substituted aryl radical or substitutionalheterocyclic aryl radical; and X and Y are independently selected from CH, N or carbon atoms connected with halogen, alkyl, oxyl, sulfenyl, amino, substituted amino, substituted aryl radical or substituted heterocyclic aryl radical. The C3/C3 fluoroquinolone dimmer derivative using oxadiazole as a connection chain can be used for preparing medicaments for treating tumors and preventing microbialinfection diseases.

The invention discloses a screen phenol-containing thiadiazole type antioxygen antiwear additive and a preparation method thereof, wherein the chemical name of the additive is 2-(3,5-di-tert-butyl-4-hydroxy-benzyl)thio-5-alkylthio 1,3,4-thiadiazole. According to the preparation method, 2,5-dimercapto-1,3,4-thiadiazole is adopted as a raw material, the 2,5-dimercapto-1,3,4-thiadiazole and a halogenated alkane are subjected to a nucleophilic substitution reaction under a catalyst effect to generate monoalkyl thiadiazole, and the monoalkyl thiadiazole, formaldehyde and 2,6-di-tert-butylphenol are subjected to a condensation polymerization reaction under a catalyst effect to obtain 2-(3,5-di-tert-butyl-4-hydroxy-benzyl)thio-5-alkylthio 1,3,4-thiadiazole type lubricating oil multifunction additive, wherein the additive is characterized in that good oxidation resistance, extreme pressure property, wear resistance and corrosion resistance are provided for the lubricant with the additive, and the additive can be combined with other additives to provide good synergy effects, can be adopted to partly or completely replace ZDDP, and is applicable for internal combustion engine oils and industrial lubricating oils.

Provided is a novel heterocyclic compound which can be used for a light-emitting element, as a host material of a light-emitting layer in which a light-emitting substance is dispersed. A heterocyclic compound represented by a general formula (G1) is provided. In the formula, A represents any of a substituted or unsubstituted dibenzothiophenyl group, a substituted or unsubstituted dibenzofuranyl group, and a substituted or unsubstituted carbazolyl group, R¹¹ to R¹⁹ separately represent any of hydrogen, an alkyl group having 1 to 4 carbon atoms, and a substituted or unsubstituted aryl group having 6 to 14 carbon atoms, and Ar represents a substituted or unsubstituted arylene group having 6 to 13 carbon atoms.

The invention discloses modified graphene and a preparation method thereof. The method comprises the following steps: performing oxidation treatment on natural flake graphite to obtain graphene oxide, and enabling graphene oxide to react with sulfoxide chloride to obtain graphene containing acyl chloride groups on the surface; then performing nucleophilic substitution reaction with 1,3-propane diamine, cyanuric chloride and a dihydric alcohol compound in sequence to obtain water-soluble graphene with hydroxyl groups on the surface, wherein the hydroxyl group content is 0.005-0.02%. Obtained modified graphene has relatively good water solubility, and is beneficial to stable dispersion of graphene; by adopting the characteristics of modified graphene, modified graphene can be mixed and uniformly dispersed with other concrete preparation materials very conveniently to prepare a reinforcing and toughening concrete product. In addition, operating conditions for preparing modified graphene can be easily met; moreover, modified graphene disclosed by the invention is easily-available in raw material, can be used for effectively reducing the cost and improving the economic benefits, and has relatively good application prospects.

There is provided a CRF receptor antagonist comprising a compound of the formula (I):

A-W—Ar  (I)

wherein, A is a group represented by the formula (A1) or (A2):

• (wherein, ring Aa is a 5- or 6-membered ring which may be further substituted; ring Ab is a 5- or 6-membered ring which may be further substituted; ring Ac is a 5- or 6-membered ring which may be substituted; R¹ is optionally substituted alkyl, substituted amino, substituted hydroxy, etc.; X is carbonyl, —O—, —S—, etc.; Y¹, Y² and Q are independently optionally substituted carbon or nitrogen; is a single or double bond); W is a bond, optionally substituted methylene, optionally substituted imino, —O—, —S—, etc.; Ar is optionally substituted aryl or optionally substituted heteroaryl; or a salt thereof or a prodrug thereof.

The present invention provides a compound of formula (I) for an organic electroluminescent device:

wherein X and Y are each independently selected for the group consisting of an alkyl substituted, aryl substituted or unsubstituted carbazole, indolocarbazole, triphenylsilyl and diphenylphosphine oxide represented by formula (A), (B), (C), (D) or (E),

in which R₁, R₂, and R₃ are each independently selected from the group consisting of a hydrogen, an alkyl having 1 to 15 carbons atoms, an aryl group having 6 to 15 carbons atoms, an alkyl substituted, an aryl substituted or unsubstituted triphenylsilyl, and a diphenylphosphine oxide represented by the formula (D) or (E); m and n are each independently 0 or 1, provided that m+n is 1 or more; and Ar₁ and Ar₂ are each independently selected from the group consisting of an alkyl substituted, aryl substituted or unsubstituted phenyl, tolyl, naphthyl, fluorenyl, anthracenyl, and phenanthryl.

The present invention relates to the preparation of Timisatan as one active component for antihypertensive medicine. The carboxylic ester derivative is first obtained through the nucleophilic substitution reaction between some intermediate and 4'-bromomethyl biphenyly-2-carboxylic ester, and then hydrolyzed to eliminnate protection radical and to obtain the destination product. In the technological process of the present invention, methyl radical and ethyl radical are used as protecting radical, and this facilitates and stabilizes the preparation of 4'-bromomethyl biphenylyl-2-methyl carboxylic ester and 4'-bromomethyl biphenylyl-2-ethyl carboxylic ester, and results in easy to control reaction with the intermediate, less impurity, easy elimination of protecting radical and high product yield and quality.

Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substituted or unsubstituted alkanoyl, (iv) substituted or unsubstituted alkenoyl wherein the double bond is cis, and (v) (ortho or para) carbonyl-substituted aryl; and wherein the subtituent is each an independent group or linked together thereby forming a ring; and wherein X is one or more substituted or unsubstituted group containing one or more O, N, or S atom and wherein the substituent is each an independent group or linked together thereby forming a ring; and wherein the therapeutic agent is an alcohol-containing water-insoluble steroids or another alcohol containing compounds and methods to prepare such compounds.

Provided is a novel heterocyclic compound which can be used in a light-emitting layer of a light-emitting element as a host material in which a light-emitting substance is dispersed. A heterocyclic compound represented by a general formula (G1) is provided. Any one of R¹ to R¹⁰ represents a substituent represented by a general formula (G1-1), another one of R¹ to R¹⁰ represents a substituent represented by a general formula (G1-2), and the others separately represent hydrogen, an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted phenyl group, or a substituted or unsubstituted biphenyl group. Further, α¹ and α² separately represent a substituted or unsubstituted phenylene group or a substituted or unsubstituted biphenyldiyl group, and A¹ and A² separately represent a substituted or unsubstituted carbazolyl group, a substituted or unsubstituted dibenzothiophenyl group, or a substituted or unsubstituted dibenzofuranyl group.

The invention discloses a novel strongly and weakly alkaline anion exchange resin with adsorption and ion exchange functions and a preparation method thereof, and relates to the field of anion exchange resin and a preparation process thereof. The novel anion exchange resin with the adsorption and ion exchange functions comprises a strong alkali group and a weak alkali group, the exchange capacityof strong alkali is 2.9 to 5.7meq for each gram of dry agent, and the exchange capacity of weak alkali is 2.8 to 3.2meq for each gram of dry agent. The preparation method of the resin comprises the following steps of: performing nucleophilic substitution reaction on macroporous chloromethylated polystyrene resin serving as a raw material and an alcohol amine compound, and reacting with thionyl chloride for further quaternization to obtain the strongly and weakly alkaline anion exchange resin.

A polyol pre-mix composition includes a blowing agent having a halogenated hydroolefin, a polyol, a catalyst composition, and an antioxidant. The antioxidant may be, for example, a benzene diol or a benzene triol or other polyhydroxy-substituted aromatic compound, which is optionally substituted with one or more substituents such as alkyl groups. A two-part system for producing a thermosetting foam blend includes (a) a polyisocyanate and, optionally, one or more isocyanate compatible raw materials; and (b) the polyol pre-mix composition. A method for producing a thermosetting foam blend includes combining: (a) a polyisocyanate; and (b) the polyol pre-mix composition.

The invention relates to a 5-site or 6-site substituent naphthalimide compound and antitumor applications thereof, which belongs to the fine chemical field. The compound is characterized in that various aliphatic amidogen, heterocyclic amidogen, aryl and Ar aryl are respectively introduced into the 5-site or 6-site of the naphthalimide by a nucleophilic substitution reaction to obtain small molecule compound similar to a lead compound amonafide structure. The small molecule compound has obvious inhibiting activity in vitro test on Hela and P388D1, and wherein, some compounds have stronger cytotoxicity than the amonafide under the same test conditions. In addition, the structures of the compounds take on diversity; the compounds without acetylation sites can be prevented from having the side effect similar to the amonafide; the other compounds with the acetylation sites can be prevented from having the side effect by personalized administration, therefore, the compound has medical application prospect in curing diseases related to tumors.