158380-73-5

Upstream product

• 63-91-2 L-phenylalanine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 100-52-7 benzaldehyde 
• 42807-45-4 N-benzyl-L-phenylalaninol 
• 145654-99-5 (S)-2-(benzyl-tert-butoxycarbonyl-amino)-3-phenyl-propionic acid methyl ester 
• 3182-95-4 L-Phenylalaninol 
• 99306-88-4 (2S)-2-Benzylideneamino-3-phenylpropan-1-ol 

Downstream Products

• 214912-34-2 N-benzyl-N-<(2S)-1-phenyl-3Z,5-hexadien-2-yl>-N-<2-(phenylsulfonyl)-2-propen-1-yl>amine 
• 214912-32-0 N-benzyl-N-<(2S)-1-phenyl-3E,5-hexadien-2-yl>-N-<2-(phenylsulfonyl)-2-propen-1-yl>amine 
• 1004316-38-4 (3-benzenesulfonyl-1-benzyl-4-tert-butoxycarbonylamino-2-hydroxy-5-phenyl-pentyl)-benzyl-carbamic acid tert-butyl ester 
• 168846-63-7 (2S,5S,3E)-2-[(1,1-dimethylethoxy)carbonyl]amino-5-{[(1,1-dimethylethoxy)carbonyl]-N-benzyl}amino-1,6-diphenylhex-3-ene 
• 168846-62-6 (2S,5S)-2,5-bis-<(1,1-dimethylethoxy)carbonylamino>-1,6-diphenylhex-3-ene 
• 144141-82-2 (2S,4S,5S)-2,5-bis<<(1,1-dimethylethoxy)carbonyl>amino>-1,6-diphenyl-4-hydroxyhexane 
• 129491-63-0 (2S,3R,4R,5S)-2,5-bis[(1,1-dimethylethoxy)carbonyl]amino-1,6-diphenyl-3,4-dihydroxyhexane 
• 129491-64-1 (2S,3S,4S,5S)-2,5-bis<<(tert-butyloxy)carbonyl>amino>-3,4-dihydroxy-1,6-diphenylhexane 
• 158380-76-8 N-benzyl-N-(tert-butoxycarbonyl)-L-phenylalaninal 

Relevant academic research and scientific papers

Substrate-Controlled Diastereoselectivity Reversal in NHC-Catalyzed Cross-Benzoin Reactions Using N-Boc-N-Bn-Protected α-Amino Aldehydes

The effectiveness of utilizing N-Bn-N-Boc-α-amino aldehydes in cross-benzoin reactions with heteroaromatic aldehydes is demonstrated. The reaction is both chemoselective and syn-selective, making it complementary to the anti-selective cross-benzoin reaction of NHBoc-α-amino aldehydes. Good diastereoselectivity is obtained for a variety of amino aldehydes, including nonhindered ones. A Felkin-Anh model can be used to rationalize the observed diastereoselectivity.

A practical total synthesis of hapalosin, a 12-membered cyclic depsipeptide with multidrug resistance-reversing activity, by employing improved segment coupling and macrolactonization

A practical total synthesis of hapalosin, a compound with multidrug resistance-reversing activity, has been carried out using an unprecedented macrolactonization strategy. One of the features of the new approach is the straightforward and fully stereocont

Preparation of aminoepoxides from aminoaldehydes and an in situ formed halomethyl organometallic reagent

In a method of preparing an aminoepoxide wherein a protected aminoaldehyde is reacted with a halomethyl organometallic reagent in an appropriate solvent at a temperature above -80 DEG C., wherein said halomethyl organometallic reagent is formed by reaction between an organometallic reagent and a dihalomethane, the improvement comprising flowing said protected aminoaldehyde into a mixing zone maintained at a temperature below 0 DEG C., also flowing said halomethyl organometallic reagent in said mixing zone for contacting in said mixing zone with said protected aminoaldehyde and also withdrawing from said mixing zone reaction products of said protected aminoaldehyde and said halomethyl organometallic reagent.

Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors

Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

HETEROCYCLECARBONYL AMINO ACID HYDROXYETHYLAMINO SULFONAMIDE RETROVIRAL PROTEASE INHIBITORS

Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Epoxide formation by continuous in-situ synthesis process

In a method of preparing an aminoepoxide wherein a protected aminoaldehyde is reacted with a halomethyl organometallic reagent in an appropriate solvent at a temperature above -80 DEG C., wherein said halomethyl organometallic reagent is formed by reaction between an organometallic reagent and a dihalomethane, the improvement comprising flowing said protected aminoaldehyde into a mixing zone maintained at a temperature below 0 DEG C., also flowing said halomethyl organometallic reagent in said mixing zone for contacting in said mixing zone with said protected aminoaldehyde and also withdrawing from said mixing zone reaction products of said protected aminoaldehyde and said halomethyl organometallic reagent.

Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors

Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Synthesis of benzo fused heterocyclic sulfonyl chlorides

A process for preparing a benzo fused heterocyclic sulfonyl halide comprising reacting a benzo fused heterocyclic compound with an SO3 complex in the presence of a water immiscible, non-reactive solvent, at a temperature of from about 0 DEG C. to about 75 DEG C., cooling, if necessary, to a temperature of from about -25 DEG C. to about 65 DEG C. and then adding oxalyl halide.

Bis-amino acid hydroxyethlamino sulfonamide retroviral protease inhibitors

PCT No. PCT/US96/02685 Sec. 371 Date Jan. 21, 1997 Sec. 102(e) Date Jan. 21, 1997 PCT Filed Mar. 7, 1996 PCT Pub. No. WO96/28464 PCT Pub. Date Sep. 19, 1996Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

AMINO ACID HYDROXYETHYLAMINO SULFONAMIDE RETROVIRAL PROTEASE INHIBITORS

Described herein is a retroviral protease inhibiting compound of the formula: STR1 or a pharmaceutically acceptable salt, prodrug or ester thereof.