3853 results about "Protecting group" patented technology

Method and structure for optimizing dual damascene patterning with polymeric dielectric materials are disclosed. Certain embodiments of the invention comprise polymeric sacrificial light absorbing materials (“polymer SLAM”) functionalized to have a controllable solubility switch wherein such polymeric materials have substantially the same etch rate as conventionally utilized polymeric dielectric materials, and subsequent to chemical modification of solubility-modifying protecting groups comprising the SLAM materials by thermal treatment or in-situ generation of an acid, such SLAM materials become soluble in weak bases, such as those conventionally utilized to remove materials in lithography treatments.

This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers:

wherein

• R1, R2, R3, R4, R5 is independently H, halogen, C₁–C₄ alkyl, nitro, nitrile, C₁–C₄ alkoxy, halogenated C₁–C₄ alkyl, or halogenated C₁–C₄ alkoxy, wherein at least one of R1, R3, and R5 is nitro;
• R6 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and
• B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases.

Nucleoside phosphinoamidite carboxylates and analogs are provided that have the structure of formula (III)

wherein A is hydrogen, hydroxyl, lower alkoxy, lower alkoxy-substituted lower alkoxy, halogen, SH, NH₂, azide or DL wherein D is O, S or NH and L is a heteroatom-protecting group, unsubstituted hydrocarbyl, substituted hydrocarbyl, heteroatom-containing hydrocarbyl, or substituted heteroatom-containing hydrocarbyl; B is a nucleobase; and one of R¹¹ and R¹² is a blocking group and the other is (IV) or (VI)

in which W, X, Y, Z, R¹ and n are as defined herein.

The invention discloses a method for synthesizing tyrosine kinase inhibitor PCI-32765. The method comprises the following steps of: 1) carrying out a coupled reaction between a compound 10 and a compound 15 to obtain a compound 6; 2) reacting the compound 6 with a compound 16 to obtain a compound 11 in the presence of a more ideal catalyst; 3) protecting the compound 11 to obtain a compound 12; 4) carrying out selective de-protection on the compound 12 to obtain a compound 13; 5) attacking the compound 13 which has only one position which can be attacked by a compound 17 to obtain a very pure compound 14; and 6) removing protecting groups, thus obtaining the PCI-32765. By the method, tyrosine kinase which serves as a main receptor signal of B cells can be inhibited, and the tyrosine kinase inhibitor PCI-32765 is not only capable of inhabiting the generation of hemocyte with little toxicity and side effects, but also is moderate in reaction conditions, simple to operate, convenient to purify, low in cost, environment-friendly, and suitable for large scale production.

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.

Disclosed herein are nucleotide analogs with one or more protecting groups, methods of synthesizing nucleotide analogs with one or more protecting groups and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with one or more protecting groups.

Bicyclonucleoside analogues which exhibit anti-AIDS activity and intermediates to produce oligonucleotide analogues which have anti-sense or anti-gene activity as well as in vivo stability. Compounds of the following formula (1) or their pharmaceutically acceptable salts.

wherein R¹ represents a hydrogen atom or a protecting group for a hydroxy group, R² represents an azido group or an optionally protected amino group or the like, B represents a purin-9-yl or a 2-oxo-1,2-dihydropyrimidin-1-yl group, which are optionally substituted with substituents selected from the group consisting of a halogen atom, an alkyl group having 1–6 carbon atoms, a hydroxy group, a mercapto group and an amino group.

Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N^α(ω-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N^α(ω-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

The invention relates to methods for modulating the side effects, including immunogenicity, of a protein therapeutic via derivatization with a protein protecting group using reversible or labile linkages.

The invention provides methods for synthesizing oligonucleotides using nucleoside monomers having carbonate protected hydroxyl groups that are deprotected with α-effect nucleophiles. The α-effect nucleophile irreversibly cleave the carbonate protecting groups while simultaneously oxidizing the internucleotide phosphite triester linkage to a phosphodiester linkage. The procedure may be carried out in aqueous solution at neutral to mildly basic pH. The method eliminates the need for separate deprotection and oxidation steps, and, since the use of acid to remove protecting groups is unnecessary, acid-induced depurination is avoided. Fluorescent or other readily detectable carbonate protecting groups can be used, enabling monitoring of individual reaction steps during oligonucleotide synthesis. The invention is particularly useful in the highly parallel, microscale synthesis of oligonucleotides.

The present invention provides novel thioester derivatives of thiazolyl acetic acid of the general formula (I),wherein, R1 represents H, trityl, CH3, or CRaRbCOOR3, in which Ra and Rb, independently of one another, represents hydrogen or methyl and R3 represents H or C1-C7 alkyl; and R2 represents C1-C4 alkyl or phenyl. The invention also provides a method for preparation of the thioester derivatives and reaction of the thioester derivatives with cephem carboxylic acids to produce cephalosporin antibiotic compounds having general formula (II),wherein, R1 represents H, trityl, CH3, or CRaRbCOOR3, in which Ra and Rb, independently of one another, represents hydrogen or methyl and R3 represents H or C1-C7 alkyl; R4 is CH3, -CH=CH2, CH2OCH3, CH2OCOCH3,and R5 is H or a salt or a carboxylic protecting group, comprising,acylating a compound of formula (III),wherein, R4 and R5 are defined as above, and R6 is H or trimethylsilyl;with a compound of formula (I).