摘要:
The invention relates to a process for the diastereoselective preparation of olefins via the Homer-Wadsworth-Emmons reaction, which consists in reacting at low temperature a phosphonate with a carbonyl derivative in the presence of a base in a suitable solvent, characterized in that a tris(polyoxaalkyl)amine sequestering reagent of formula (I): N—[CHR1—CHR2—O—(CHR3—CHR4—O)n—R5]3 (I), wherein: n is an integer between 0 and 10; R1, R2, R3 and R4 may be identical or different, and represent a hydrogen atom or an alkyl radical containing from 1 to 4 carbon atoms; R5 represents a hydrogen atom, an alkyl or cycloalkyl radical containing up to 12 carbon atoms, a phenyl radical or a radical of formula —CμH2μ-Φ, or CmH2m+1-Φ-, with m being an integer between 1 and 12 and Φ being a phenyl radical; is added in an amount that is sufficient to increase the diastereoselectivity of the olefin.
摘要翻译:本发明涉及通过Homer-Wadsworth-Emmons反应非对映选择性制备烯烃的方法,该方法在低温下使膦酸酯与羰基衍生物在碱的存在下在合适的溶剂中反应,其特征在于三 (I)的(多氧烷基)胺螯合试剂:N- [CHR 1 -CH 2,-SO 2 -O-(CHR 3 - (I)其中:n是介于0和...之间的整数,其中,n是0和...之间的整数。 10; R 1,R 2,R 3和R 4可以相同或不同,并且表示氢原子 或含有1至4个碳原子的烷基; R 5表示氢原子,含有至多12个碳原子的烷基或环烷基,苯基或式-CmuH 2 mu-Phi的基团或C m H 2m + 1 -hi-,m是1和12之间的整数,Phi是苯基; 以足以增加烯烃的非对映选择性的量加入。
摘要:
The invention relates to a method of preparing an acylimidazolium-type reagent. More specifically, the invention relates to a salt of N-(benzyloxycarbonyl)-N′-methylimidazolium. The inventive method of preparing an acylimidazolium-type reagent is characterised in that it is obtained by: (i) reacting a reagent comprising a —COX group having formula (II) and an imidazole reagent having formula (III); and (ii) subsequently, adding a strong acid HY to the product thus obtained, said acid having a pKa of less than 1, which produces the desired reagent.
摘要:
The present invention concerns a process for preparing a polyaromatic compound comprising a concatenation of two aromatic cycles and carrying at least one amino group on one of the aromatic cycles. The process of the invention is characterized in that it consists of reacting an aromatic compound carrying at least one amino group and a leaving group with an arylboronic acid in an aqueous medium and in the presence of a palladium catalyst.
摘要:
This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.
摘要:
The invention concerns novel nitroaromatic compounds of general formula (I′) wherein: R, R′1, R2, Z and n are as defined in claim 38. The invention also concerns a method for preparing nitroaromatic compounds nitrated in position 4. The invention further concerns the use of said compounds for preparing heterocyclic benzofuran or benzothiophene derivatives nitrated in position 5. The invention concerns particularly the preparation of 2-alkyl-5-nitrobezofuran
摘要:
This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.
摘要:
The present invention relates to a method of preparation of an alkyne with an optically active hydroxyl group in the β or γ position of a triple bond and intermediates obtained. The method of the invention for preparation of an alkyne with an optically active hydroxyl group in the β position of a triple bond is characterized in that it comprises the reaction, in the presence of a Lewis acid: of a compound of formula (IV): in which: R is a linear or branched alkyl group having from 1 to 6 carbon atoms. and of a compound of formula (V): R′—C≡C-M (V) in which: R′ represents a hydrogen atom, a linear or branched alkyl group having from 1 to 8 carbon atoms, preferably a methyl group or a trialkylsilyl group. M represents a metal, preferably a metal of group (Ia) of the periodic table, preferably lithium. Another object of the invention comprises the production of an alkyne with an optically active hydroxyl group in the γ position of a triple bond by isomerization of an alkyne with an optically active hydroxyl group in the β position previously obtained.
摘要:
The invention concerns a method for preparing aromatic diphenyl thioethers. More particularly the invention concerns the preparation of 4-chloro-4′-thiomethyldiphenylether. The inventive method for preparing an aromatic diphenyl thioether is characterised in that it consists in reacting in an aqueous medium a diazonium salt of an aromatic diphenyl compound with a disulphide sulphur compound, in the presence of an efficient amount of a coupling catalyst.
摘要:
The invention relates to a method for the production of a compound comprising a free hydroxyl group and a hydroxyl group which is protected by an ester function by enzymatic reaction, using a lipase EC 3.1.1.3. The invention also relates to the use of the resultant compound as an intermediate for the production of medicaments and pharmaceutical products.
摘要:
The invention concerns novel nitroaromatic compounds of general formula (I′) wherein: R, R′1, R2, Z and n are as defined in claim 1. The invention also concerns a method for preparing nitroaromatic compounds nitrated in position 4. The invention further concerns the use of said compounds for preparing heterocyclic benzofuran or benzothiophene derivatives nitrated in position 5. The invention concerns particularly the preparation of 2-alkyl-5-nitrobezofuran.