Abstract: A method for preparing an oligonucleotide comprising the steps of synthesizing a phosphoramidite by reacting a hydroxyl-containing compound of formula (A) with a phosphitylating agent in the presence of an activator compound of formula (I), to prepare a phosphitylated compound, then coupling the phosphitylated compound without isolation with a second compound having the formula (A), wherein R5, R3, R2, B are independently selected, but have the same definition as above in the presence of an activator II selected from the group of imidazole, imidazolium salts, and mixtures thereof, which are improved activators over activators disclosed in related art.

Abstract: A method for purifying a protected oligonucleotide comprising the steps of: a) providing a solution of the protected oligonucleotide in at least one solvent A having a boiling point below the boiling point of a solvent B, heating the solution at a temperature of at least 30° C. and below the boiling point of the at least solvent A, adding solvent B until precipitation of a material is visible in the solution, said solvent B being an alcohol having 1 to 6 C-atoms or a diol having 2 to 6 C-atoms, allowing the solution to cool down under stirring until formation of a supernatant and a residue, removing the supernatant or b) providing solvent B, said solvent B being an alcohol having 1 to 6 C-atoms or a diol having 2 to 6 C-atoms, heating solvent B at a temperature above 30° C.

Abstract: A method for preparing an oligonucleotide comprising the steps of a) providing a hydroxyl containing compound having the formula (A), b) reacting said compound with a phosphitylating agent in the presence of an activator (activator I) having the formula (I) to prepare a phosphitylated compound; and c) reacting said phosphitylated compound without isolation with a second compound having the formula (A) wherein R5, R3, R2, B are independently selected, but have the same definition as above in the presence of an activator II different from activator I.

Abstract: A method for preparing a phosphitylated compound comprising the step of:—reacting a hydroxyl containing compound with a phosphitylating agent in the presence of an activator having the formula (I) wherein R=alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl R1, R2=either H or form a 5 to 6-membered ring together. X1, X2=independently either N or CH Y?H or Si(R4)3, with R4=alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl B=deprotonated acid. The hydroxyl containing compound is preferably a sugar moiety or a nucleoside or an oligomer derived therefrom.

Abstract: A solution phase synthesis method for preparing an oligonucleotide, wherein at least some of the reagents are solid supported. The method suitable for large-scale synthesis comprises coupling a protected compound with a nucleotide derivative having a protection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond; optionally processing the elongated oligonucleotide by capping by reaction with a solid supported capping agent and/or by oxidizing or sulfurizing by reaction of the oligonucleotide with a solid supported oxidizing or sulfurization reagent; and removing the protection group. The coupling may include reacting a 3?-protected compound of formula: with a nucleotide derivative having a 5?-protection group, or reacting a 5?-protected compound of formula with a nucleotide derivative having a 3?-protection group.

Abstract: A solution phase synthesis method for preparing an oligonucleotide, wherein at least some of the reagents are solid supported. The method suitable for large- scale synthesis comprises coupling a protected compound with a nucleotide derivative having a protection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond; optionally processing the elongated oligonucleotide by capping by reaction with a solid supported capping agent and/or by oxidizing or sulfurizing by reaction of the oligonucleotide with a solid supported oxidizing or sulfurization reagent; and removing the protection group. The coupling may include reacting a 3?-protected compound of formula: with a nucleotide derivative having a 5?-protection group, or reacting a 5?-protected compound of formula with a nucleotide derivative having a 3?-protection group.

Abstract: A method for preparing an oligonucleotide comprising the steps of a) providing a hydroxyl containing compound having formula (1), wherein B is a heterocyclic base, and radicals R2, R3 and R5 are as defined in the description; b) reacting said compound with a phosphitylating agent in the presence of an activator I having formula (I), wherein R=alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl; R1, R2=either H or form a 5- to 6-membered ring together; X1, X2=independently either N or CH; Y=H or Si(R4)3, with R4=alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl; B=deprotonated acid; to prepare a phosphitylated compound; c) reacting said phosphitylated compound without isolation with a second compound having the formula (1), wherein R5, R3, R2, B are independently selected, but have the same definition as above in the presence of an activator II selected from the group of imidazole, imidazolium salts, and mixtures thereof.

Abstract: A method for preparing an oligonucleotide comprising the steps of a) providing a hydroxyl containing compound having the formula (A), b) reacting said compound with a phosphitylating agent in the presence of an activator (activator I) having the formula (I) to prepare a phosphitylated compound; and c) reacting said phosphitylated compound without isolation with a second compound having the formula (A) wherein R5, R3, R2, B are independently selected, but have the same definition as above in the presence of an activator II different from activator I.

Abstract: A process for the synthesis of compounds of general formulas comprising the step of reacting in the presence of wherein: R=substituted or unsubstituted alkyl, aryl, heterocycles containing one or more O, N, S, P or B; R1 and R2 independently represent H, substituted or unsubstituted alkyl, aryl, heterocycles containing one or more O, N, S, P or B; R?=H, OH, OR or OSiX3, wherein X independently represent alkyl or aryl.

Abstract: A method for purifying a protected oligonucleotide comprising the steps of: a) providing a solution of the protected oligonucleotide in at least one solvent A having a boiling point below the boiling point of a solvent B, heating the solution at a temperature of at least 30° C. and below the boiling point of the at least solvent A, adding solvent B until precipitation of a material is visible in the solution, said solvent B being an alcohol having 1 to 6 C-atoms or a diol having 2 to 6 C-atoms, allowing the solution to cool down under stirring until formation of a supernatant and a residue, removing the supernatant or b) providing solvent B, said solvent B being an alcohol having 1 to 6 C-atoms or a diol having 2 to 6 C-atoms, heating solvent B at a temperature above 30° C.

Abstract: A solution phase synthesis method for preparing an oligonucleotide, wherein at least some of the reagents are solid supported. The method suitable for large-scale synthesis comprises coupling a protected compound with a nucleotide derivative having a protection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond; optionally processing the elongated oligonucleotide by capping by reaction with a solid supported capping agent and/or by oxidizing or sulfurizing by reaction of the oligonucleotide with a solid supported oxidizing or sulfurization reagent; and removing the protection group. The coupling may include reacting a 3?-protected compound of formula: with a nucleotide derivative having a 5?-protection group, or reacting a 5?-protected compound of formula with a nucleotide derivative having a 3?-protection group.

Abstract: A process for the synthesis of compounds of general formulas comprising the step of reacting in the presence of wherein: R=substituted or unsubstituted alkyl, aryl, heterocycles containing one or more O, N, S, P or B; R1 and R2 independently represent H, substituted or unsubstituted alkyl, aryl, heterocycles containing one or more O, N, S, P or B; R??H, OH, OR or OSiX3, wherein X independently represent alkyl or aryl.

Abstract: A method for preparing an oligonucleotide comprising the steps of a) providing a 3-protected compound having the formula: wherein B is a heterocyclic base R2 is H, a protected 2-hydroxyl group, F, a protected amino group, an O-alkyl group, an O-substituted alkyl, a substituted alkylamino or a C4?-O2?methylen linkage R3 is OR?3, NHR?3, NR?3R??3, a 3?-protected nucleotide or a 3?-protected oligonucleotide, R?3 is a hydroxyl protecting group, R?3, R??3 are independently an amine protecting group, b) reacting said compound with a nucleotide derivative having a 5-proctection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond c) optionally processing the elongated oligonucleotide with a P(III)-internucleotide bond by either or both of steps c1) and c2) in any sequence c1) capping preferably by reacting with a solid supported capping agent c2) oxidizing preferably by reacting the oligonucleotide with a solid supported oxidizing reagent d) remo

Abstract: The present invention relates to peptide compounds comprising two single-chain hemoregulatory, for example haemopoiesis-inhibiting, peptides linked by a bridging group terminally attached to the C.alpha. atoms of non-terminal amino acids wherein at least one of the C.alpha. atoms is independently substituted by an alkyl group. The bridged dipeptide compounds have a stimulating activity on cell division, especially in myelopoietic and bone marrow cells.

Abstract: Dipeptide compounds are disclosed, the two peptide chains being joined together at a C.alpha.-atom of a non-terminal amino acid by a divalent bridging group --A--. The C.alpha.-atoms joined to group --A-- are located in equivalent positions in each peptide and each lack their native .alpha.-side chain. The bridged dipeptide compounds disclosed have a stimulating activity on cell division, especially for myelopoietic and bone marrow cells.

Abstract: Process for producing dipeptides from non-proteinogenic amino acids with terminal carbon atoms.

Abstract: A process for preparing dipeptides with N-terminal non-proteinogenous amino acids of the formula ##STR1## in which R.sup.1 to R.sup.6 have the meaning stated in the description, from compounds of the formula ##STR2## is described.