Patent classifications
C07C381/00
Integrin antagonist conjugates for targeted delivery to cells expressing LFA-1
The invention relates to compounds of formula (I), wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1. ##STR00001##
Method for producing polythiol compound, polymerizable composition for optical material, and uses thereof
Provided is a method for producing a molded product comprising a step for preparing a polymerizable composition for optical materials and a step for curing the polymerizable composition for optical materials to produce the molded product. The step for preparing the polymerizable composition for optical materials comprises a step for preparing a defined polythiol compound and a step for preparing the polymerizable composition for optical materials from the polythiol compound. The step for preparing the defined polythiol compound comprises reacting 2-mercaptoethanol with a defined epihalohydrin compound at a temperature of 10 C. to 50 C. to obtain a defined polyalcohol compound, reacting the polyalcohol compound with thiourea in the presence of hydrogen chloride to obtain an isothiuronium salt, hydrolyzing the isothiuronium salt to obtain the polythiol compound, adding hydrochloric acid at a defined concentration to a solution of the polythiol compound, and washing the solution to purify the polythiol compound.
Method for producing polythiol compound, polymerizable composition for optical material, and uses thereof
Provided is a method for producing a molded product comprising a step for preparing a polymerizable composition for optical materials and a step for curing the polymerizable composition for optical materials to produce the molded product. The step for preparing the polymerizable composition for optical materials comprises a step for preparing a defined polythiol compound and a step for preparing the polymerizable composition for optical materials from the polythiol compound. The step for preparing the defined polythiol compound comprises reacting 2-mercaptoethanol with a defined epihalohydrin compound at a temperature of 10 C. to 50 C. to obtain a defined polyalcohol compound, reacting the polyalcohol compound with thiourea in the presence of hydrogen chloride to obtain an isothiuronium salt, hydrolyzing the isothiuronium salt to obtain the polythiol compound, adding hydrochloric acid at a defined concentration to a solution of the polythiol compound, and washing the solution to purify the polythiol compound.
Industrial methods for producing arylsulfur pentafluorides
Industrial methods for producing arylsulfur pentafluorides are disclosed. Methods include reacting arylsulfur halotetrafluoride with hydrogen fluoride in the absence or presence of one or more additives selected from a group of fluoride salts, non-fluoride salts, and unsaturated organic compounds to form arylsulfur pentafluorides.
Industrial methods for producing arylsulfur pentafluorides
Industrial methods for producing arylsulfur pentafluorides are disclosed. Methods include reacting arylsulfur halotetrafluoride with hydrogen fluoride in the absence or presence of one or more additives selected from a group of fluoride salts, non-fluoride salts, and unsaturated organic compounds to form arylsulfur pentafluorides.
Industrial methods for producing arylsulfur pentafluorides
Industrial methods for producing arylsulfur pentafluorides are disclosed. Methods include reacting arylsulfur halotetrafluoride with hydrogen fluoride in the absence or presence of one or more additives selected from a group of fluoride salts, non-fluoride salts, and unsaturated organic compounds to form arylsulfur pentafluorides.
Industrial methods for producing arylsulfur pentafluorides
Industrial methods for producing arylsulfur pentafluorides are disclosed. Methods include reacting arylsulfur halotetrafluoride with hydrogen fluoride in the absence or presence of one or more additives selected from a group of fluoride salts, non-fluoride salts, and unsaturated organic compounds to form arylsulfur pentafluorides.
Method for producing polythiol compound, polymerizable composition for optical material, and uses thereof
Provided is a method for producing a molded product comprising preparing a polymerizable composition for optical materials and curing the polymerizable composition for optical materials to produce the molded product. The preparation of the polymerizable composition comprises preparing a polythiol compound containing, as a main component, one kind or two or more kinds selected from a defined group of compounds, and preparing the polymerizable composition from the polythiol compound. The preparation of the polythiol compound comprises reacting 2-mercaptoethanol with a defined epihalohydrin compound to obtain a defined compound, reacting the defined compound with sodium sulfide to obtain a defined polyalcohol compound, reacting the polyalcohol compound with thiourea in the presence of hydrogen chloride to obtain an isothiuronium salt, adding aqueous ammonia to a reaction solution containing the isothiuronium salt thereby hydrolyzing the isothiuronium salt to obtain the polythiol compound and purifying the polythiol compound with hydrochloric acid.
Method for producing polythiol compound, polymerizable composition for optical material, and uses thereof
Provided is a method for producing a molded product comprising preparing a polymerizable composition for optical materials and curing the polymerizable composition for optical materials to produce the molded product. The preparation of the polymerizable composition comprises preparing a polythiol compound containing, as a main component, one kind or two or more kinds selected from a defined group of compounds, and preparing the polymerizable composition from the polythiol compound. The preparation of the polythiol compound comprises reacting 2-mercaptoethanol with a defined epihalohydrin compound to obtain a defined compound, reacting the defined compound with sodium sulfide to obtain a defined polyalcohol compound, reacting the polyalcohol compound with thiourea in the presence of hydrogen chloride to obtain an isothiuronium salt, adding aqueous ammonia to a reaction solution containing the isothiuronium salt thereby hydrolyzing the isothiuronium salt to obtain the polythiol compound and purifying the polythiol compound with hydrochloric acid.
Methods for the synthesis of functionalized nucleic acids
The present application, among other things, provides technologies, e.g., reagents, methods, etc. for preparing oligonucleotides comprising phosphorothiotriesters linkages, e.g., oligonucleotides having the structure of IIIa, IIIb or IIIc. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ia or Ib with a silylating reagent to provide a silyloxyphosphonate, and reacting the silyloxyphosphonate with a thiosulfonate reagent of structure IIa or IIb to provide an oligonucleotide of structure IIIa or IIIb. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ic with a silylating reagent to provide a silyloxyphosphonate, reacting the silyloxyphosphonate with a bis(thiosulfonate) reagent of structure IVc to provide a phosphorothiotriester comprising a thiosulfonate group of structure Vc, and then reacting the phosphorothiotriester comprising a thiosulfonate group of structure Vc with a nucleophile of structure VIc to provide an oligonucleotide of structure IIIc.