Y02P20/55

BETA-LACTAM COMPOUND, USE THEREOF AND PREPARATION METHOD THEREFOR

The present invention relates to a compound as shown in general formula (I) below (in formula (I), each of R.sub.1 and R.sub.2 independently represents a hydrogen atom or a C1-10 linear or branched alkyl optionally having a substituent, or the two together form a cycloalkyl with 3 to 8 ring carbon atoms; each of R.sub.3 and R.sub.4 independently represents a hydrogen atom or a C1-10 linear or branched alkyl optionally having a substituent or a C6-12 aryl optionally having a substituent, or the two together form a cycloalky with 3 to 8 ring carbon atoms; X represents C or N; and Y represents a linear or branched alkenyl or alkynyl with 2 to 6 carbon atoms and optionally having a substituent, or carboxyl). The compound has good antibacterial properties against bacteria, especially gram-negative bacteria, has low drug resistance, and has good prospects for the effective treatment of various conditions.

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MULTI-SIGNAL FLUORESCENT PROBE FOR EARLY DIAGNOSIS OF TUMORS, AND PREPARATION AND USE THEREOF
20230226226 · 2023-07-20 ·

A multi-signal fluorescent probe, represented by:

##STR00001##

A method for preparing the multi-signal fluorescent probe includes: (a) adding 2-methoxyphenothiazine and ethyl iodide into a mixture of dichloromethane (DCM) and acetonitrile followed by a first reaction and a first post-treatment to obtain 10-ethyl-2-methoxy-10H-phenothiazine; (b) adding boron tribromide into the 10-ethyl-2-methoxy-10H-phenothiazine under an inert gas followed by a second reaction under an ice bath and a second post-treatment to obtain 10-ethyl-10H-phenothiazin-2-ol; and (c) mixing the 10-ethyl-10H-phenothiazin-2-ol, malonic acid, zinc chloride and phosphorus oxychloride followed by a third reaction and a third post-treatment to obtain the multi-signal fluorescent probe. A use of the multi-signal fluorescent probe in the detection of intracellular ONOO.sup.- and Na.sub.2S.sub.2 is also provided.

Process for preparing mannose derivatives

The invention relates to a process to prepare a compound of the following formula (I): (I), in which P represents a protective group of a hydroxyl function which is a —COR.sup.1 group with R.sup.1 representing an aryl or a (C.sub.1C.sub.6)alkyl, R represents a hydrogen atom or a protective group of a terminal alkyne, from mannose, comprising the following steps: (a) protecting the 5 hydroxyl groups of the mannose by a protective group P; (b) coupling the protected mannose obtained at step (a) with a compound of the following formula (II). The present invention also relates to a compound of formula (IIIa). ##STR00001##

Method for preparing oligonucleic acid compound

A method for subjecting a compound [A] having a hydroxyl group or a primary or secondary amino group and a compound [B] having a substituent containing a phosphorus atom to a condensation reaction to prepare a compound [C] represented by the following general formula [C]: ##STR00001##
wherein the condensation reaction is carried out in a mixed solvent containing a polar solvent and a halogen solvent as a reaction solvent.

METHOD FOR PRODUCING 3,6-DISUBSTITUTED-IMIDAZO[1,2-B]PYRIDAZINE DERIVATIVE
20230227459 · 2023-07-20 ·

This disclosure relates to a crystal of 3-{4-[(2R)-2-aminopropoxy]phenyl}-N-[(1R)-1-(3-fluorophenyl)ethyl]imidazo[1,2-b]pyridazin-6-amine adipate.

Site-specific antibody-drug conjugates

Site-specific antibody-drug conjugates are described, in particular conjugates comprising pyrrolobenzodiazepines (PBDs) having a labile protecting group in the form of a linker. The site of conjugation, along with modification of the antibody moiety, allows for improved safety and efficacy of the ADC.

Method for preparing trifluridine

The present application relates to a method for preparing trifluridine, comprising reacting a compound of formula III with a compound of formula IV in a first solvent in the presence of an acid to obtain a compound of formula II, and performing further reaction to obtain trifluridine.

PROCESS AND INTERMEDIATE FOR THE PREPARATION OF OXETAN-2-YL-METHANAMINE
20230013840 · 2023-01-19 ·

A process and intermediate for the preparation of a compound of formula (I), or salt thereof.

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METHOD FOR PRODUCING OLIGONUCLEIC ACID COMPOUND
20230014840 · 2023-01-19 · ·

The present invention relates to a method for producing a compound represented by general formula [C-1-1], which comprises: a step for reacting a compound represented by general formula [B-1-1] with a compound represented by general formula [P] to form a compound represented by general formula [B-1-2]; and a step for reacting the compound represented by general formula [B-1-2] with a compound represented by general formula [A-1] to form the compound represented by general formula [C-1-1].

METHOD FOR PRODUCING OLIGONUCLEIC ACID COMPOUND
20230018780 · 2023-01-19 · ·

The present invention relates to a method for producing a compound [C] of the general formula [C] by subjecting a compound [A] having a hydroxyl group or a primary or secondary amino group and a compound [B] having a phosphorous atom-containing substituent group of the general formula [1] to a condensation reaction, characterized in that the method is carried out in the presence of at least one reaction accelerator selected from the group consisting of a quaternary ammonium salt, a quaternary imidazolium salt, a quaternary morpholinium salt, a quaternary phosphonium salt, a quaternary piperidinium salt, a quaternary pyridinium salt, a quaternary pyrrolidinium salt and a quaternary sulfonium salt.